DT-Web: DB00598

Identification

Name

Labetalol

Accession Number

DB00598 (APRD01062)

Type

small molecule

Description

Blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive. [PubChem]

Structure

MOL SDF PDB SMILES InChI

Categories ^(*)

Molecular Weight

328.4055

Groups

approved

Monoisotopic Weight

328.178692644

Pharmacology

Indication

For the management of hypertension (alone or in combination with other classes of antihypertensive agents), as well as chronic stable angina pectoris and sympathetic overactivity syndrome associated with severe tetanus. Labetalol is used parenterally for immediate reduction in blood pressure in severe hypertension or in hypertensive crises when considered an emergency, for the control of blood pressure in patients with pheochromocytoma and pregnant women with preeclampsia, and to produce controlled hypotension during anesthesia to reduce bleeding resulting from surgical procedures.

Mechanism of action

Labetalol HCl combines both selective, competitive, alpha-1-adrenergic blocking and nonselective, competitive, beta-adrenergic blocking activity in a single substance. In man, the ratios of alpha- to beta- blockade have been estimated to be approximately 1:3 and 1:7 following oral and intravenous (IV) administration, respectively. The principal physiologic action of labetalol is to competitively block adrenergic stimulation of ?-receptors within the myocardium (?1-receptors) and within bronchial and vascular smooth muscle (?2-receptors), and ?1-receptors within vascular smooth muscle. This causes a decrease in systemic arterial blood pressure and systemic vascular resistance without a substantial reduction in resting heart rate, cardiac output, or stroke volume, apparently because of its combined ?- and ?-adrenergic blocking activity.

Absorption

Completely absorbed (100%) from the gastrointestinal tract with peak plasma levels occurring 1 to 2 hours after oral administration. The absolute bioavailability of labetalol is increased when administered with food.

Protein binding

50%

Biotransformation

Primarily hepatic, undergoes significant first pass metabolism

Route of elimination

These metabolites are present in plasma and are excreted in the urine, and via the bile, into the feces.

Toxicity

LD₅₀ = 66 mg/kg (Rat, IV). Side effects or adverse reactions include dizziness when standing up, very low blood pressure, severely slow heartbeat, weakness, diminished sexual function, fatigue

Affected organisms

Humans and other mammals

Interactions

Drug Interactions

Drug	Mechanism of interaction
Acetohexamide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Chlorpropamide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Cimetidine	Cimetidine may increase the serum concentration of labetolol by decreasing its metabolism.
Clonidine	Increased hypertension when clonidine stopped
Dihydroergotamine	Ischemia with risk of gangrene
Dihydroergotoxine	Ischemia with risk of gangrene
Disopyramide	The beta-blocker, labetolol, may increase the toxicity of disopyramide.
Enflurane	Monitor arterial pressure closely
Epinephrine	Hypertension, then bradycardia
Ergonovine	Ischemia with risk of gangrene
Ergotamine	Ischemia with risk of gangrene
Fenoterol	Antagonism
Formoterol	Antagonism
Gliclazide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Glipizide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Glisoxepide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Glyburide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Glycodiazine	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Halothane	Monitor arterial pressure closely
Ibuprofen	Risk of inhibition of renal prostaglandins
Indomethacin	Risk of inhibition of renal prostaglandins
Insulin Glargine	The beta-blocker, labetolol, may decrease symptoms of hypoglycemia.
Iobenguane	May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it depletes or inhibit reuptake of noradrenaline stores
Isoflurane	Monitor arterial pressure closely
Isoproterenol	Antagonism
Lidocaine	The beta-blocker, labetalol, may increase the effect and toxicity of lidocaine.
Methysergide	Ischemia with risk of gangrene
Orciprenaline	Antagonism
Pipobroman	Antagonism
Pirbuterol	Antagonism
Piroxicam	Risk of inhibition of renal prostaglandins
Prazosin	Risk of hypotension at the beginning of therapy
Procaterol	Antagonism
Repaglinide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Salbutamol	Antagonism
Salmeterol	Antagonism
Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Terbutaline	Antagonism
Tolazamide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Tolbutamide	The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Verapamil	Increased effect of both drugs

Food Interactions

Take without regard to meals.

Beta-1 adrenergic receptor
Name	Beta-1 adrenergic receptor
Gene Name	ADRB1
Pharmacological action	yes
Actions	antagonist
References	Riva E, Mennini T, Latini R: The alpha- and beta-adrenoceptor blocking activities of labetalol and its RR-SR (50:50) stereoisomers. Br J Pharmacol. 1991 Dec;104(4):823-8. - Pubmed Monopoli A, Bamonte F, Forlani A, Ongini E, Parravicini L: Effects of the R, R-isomer of labetalol, SCH 19927, in isolated tissues and in spontaneously hypertensive rats during a repeated treatment. Arch Int Pharmacodyn Ther. 1984 Dec;272(2):256-63. - Pubmed Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. - Pubmed Nakagawa Y, Takeda K, Sakurai H, Mitomi A, Imai S: [Antihypertensive effects of labetalol in three types of hypertensive models of rats (author's transl)] Nippon Yakurigaku Zasshi. 1981 Apr;77(4):435-45. - Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed Pujos E, Cren-Olive C, Paisse O, Flament-Waton MM, Grenier-Loustalot MF: Comparison of the analysis of beta-blockers by different techniques. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Dec 1;877(31):4007-14. Epub 2009 Oct 17. - Pubmed Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. - Pubmed van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. - Pubmed
DTHybrid score	0.7342
Beta-2 adrenergic receptor
Name	Beta-2 adrenergic receptor
Gene Name	ADRB2
Pharmacological action	yes
Actions	antagonist
References	Doggrell SA: The effects of labetalol and dilevalol on isolated cardiovascular preparations of the guinea-pig and rat. J Pharm Pharmacol. 1992 Dec;44(12):1001-6. - Pubmed Doggrell SA: Relaxant and beta 2-adrenoceptor blocking activities of labetalol, dilevalol, amosulalol and KF-4317 on the rat isolated aorta. J Pharm Pharmacol. 1988 Nov;40(11):812-5. - Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. - Pubmed Pujos E, Cren-Olive C, Paisse O, Flament-Waton MM, Grenier-Loustalot MF: Comparison of the analysis of beta-blockers by different techniques. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Dec 1;877(31):4007-14. Epub 2009 Oct 17. - Pubmed Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. - Pubmed van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. - Pubmed
DTHybrid score	0.742
Alpha-1A adrenergic receptor
Name	Alpha-1A adrenergic receptor
Gene Name	ADRA1A
Pharmacological action	yes
Actions	antagonist
References	Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. - Pubmed Pedersen ME, Cockcroft JR: The vasodilatory beta-blockers. Curr Hypertens Rep. 2007 Aug;9(4):269-77. - Pubmed Shiraishi K, Moriya M, Miyake N, Takayanagi I: Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes? Gen Pharmacol. 1992 Sep;23(5):843-5. - Pubmed Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. - Pubmed van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. - Pubmed
DTHybrid score	0.4485
Alpha-1B adrenergic receptor
Name	Alpha-1B adrenergic receptor
Gene Name	ADRA1B
Pharmacological action	yes
Actions	antagonist
References	Bernstein JS, Ebert TJ, Stowe DF, Schmeling WT, Nelson MA, Woods MP: Partial attenuation of hemodynamic responses to rapid sequence induction and intubation with labetalol. J Clin Anesth. 1989;1(6):444-51. - Pubmed Nakamura T, Maruyama K, Ohnuki T, Hattori K, Watanabe K, Nagatomo T: Tamsulosin: assessment of affinityof (3)H-P razosin binding to two alpha-1- adrenoceptor subtypes in the canine aorta. Pharmacology. 1999 Nov;59(5):234-8. - Pubmed Sassard J, Zech PY, Pozet N, Cuisinaud G, Vincent M: [Comparative effects of an alpha 1 and beta 1-2 blocker (labetalol) and a beta-1 blocker (atenolol) in the hypertensive patient] J Pharmacol. 1983;14 Suppl 2:121-9. - Pubmed Pedersen ME, Cockcroft JR: The vasodilatory beta-blockers. Curr Hypertens Rep. 2007 Aug;9(4):269-77. - Pubmed Shiraishi K, Moriya M, Miyake N, Takayanagi I: Alpha 1-adrenoceptor blocking activities of bevantolol hydrochloride(NC-1400) and labetalol in rat isolated thoracic aorta--do they distinguish between subtypes? Gen Pharmacol. 1992 Sep;23(5):843-5. - Pubmed Rosendorff C: Beta-blocking agents with vasodilator activity. J Hypertens Suppl. 1993 Jun;11(4):S37-40. - Pubmed van Zwieten PA: An overview of the pharmacodynamic properties and therapeutic potential of combined alpha- and beta-adrenoceptor antagonists. Drugs. 1993 Apr;45(4):509-17. - Pubmed
DTHybrid score	0.295

Cytochrome P450 2D6
Name	Cytochrome P450 2D6
Gene Name	CYP2D6
Actions	substrate,inhibitor
References	Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. - Pubmed
DTHybrid score	0.3914

Id	Partner name	Gene Name	Score
4512	Cytochrome P450 3A4	CYP3A4	0.1704
318	Alpha-2A adrenergic receptor	ADRA2A	0.1578
1517	Beta-3 adrenergic receptor	ADRB3	0.1445
789	Alpha-1D adrenergic receptor	ADRA1D	0.1368
1588	Multidrug resistance protein 1	ABCB1	0.1277
4200	Cytochrome P450 1A2	CYP1A2	0.1093
320	5-hydroxytryptamine 1A receptor	HTR1A	0.1055
540	Sodium-dependent noradrenaline transporter	SLC6A2	0.0961
6016	Cytochrome P450 2C19	CYP2C19	0.0882
831	D(2) dopamine receptor	DRD2	0.0854
502	5-hydroxytryptamine 2A receptor	HTR2A	0.0852
23	D(1A) dopamine receptor	DRD1	0.0804
629	Alpha-2B adrenergic receptor	ADRA2B	0.0759
4757	Cytochrome P450 2C9	CYP2C9	0.0751
492	Histamine H1 receptor	HRH1	0.0682
713	Sodium-dependent dopamine transporter	SLC6A3	0.0643
378	Alpha-2C adrenergic receptor	ADRA2C	0.0637
101	Potassium voltage-gated channel subfamily H member 2	KCNH2	0.0629
1181	Alpha-1-acid glycoprotein 1	ORM1	0.0557
824	Sodium-dependent serotonin transporter	SLC6A4	0.054
4118	Cytochrome P450 3A5	CYP3A5	0.0518
6145	Solute carrier family 22 member 1	SLC22A1	0.0512
6144	Solute carrier family 22 member 2	SLC22A2	0.0511
885	5-hydroxytryptamine 1B receptor	HTR1B	0.0503
590	5-hydroxytryptamine 2C receptor	HTR2C	0.0481
103	Muscarinic acetylcholine receptor M1	CHRM1	0.0433
6107	Cytochrome P450 3A7	CYP3A7	0.0416
3923	Cholinesterase	BCHE	0.0412
4924	Cytochrome P450 2C8	CYP2C8	0.041
6024	Cytochrome P450 1A1	CYP1A1	0.0409
131	Synaptic vesicular amine transporter	SLC18A2	0.0404
6013	Cytochrome P450 2E1	CYP2E1	0.0395
6030	Cytochrome P450 2B6	CYP2B6	0.0384
3941	Amine oxidase [flavin-containing] A	MAOA	0.0379
432	D(4) dopamine receptor	DRD4	0.0364
274	Muscarinic acetylcholine receptor M5	CHRM5	0.0324
51	Muscarinic acetylcholine receptor M3	CHRM3	0.0323
450	Muscarinic acetylcholine receptor M4	CHRM4	0.0315
638	D(3) dopamine receptor	DRD3	0.0312
617	Muscarinic acetylcholine receptor M2	CHRM2	0.03
5718	Cytochrome P450 2A6	CYP2A6	0.0274
828	Phenylalanine-4-hydroxylase	PAH	0.0269
3109	Phenylalanine-4-hydroxylase	phhA	0.0269
2300	Lysozyme	E	0.0253
3633	Lysozyme	R	0.0253
5597	Lysozyme	17	0.0253
725	5-hydroxytryptamine 1D receptor	HTR1D	0.0251
587	Serum albumin	ALB	0.0235
118	Organic cation/carnitine transporter 2	SLC22A5	0.0231
1256	5-hydroxytryptamine 6 receptor	HTR6	0.023
514	Potassium voltage-gated channel subfamily H member 6	KCNH6	0.0218
772	Potassium voltage-gated channel subfamily H member 7	KCNH7	0.0217
163	D(1B) dopamine receptor	DRD5	0.0214
3810	Catechol O-methyltransferase	COMT	0.0214
6147	Solute carrier family 22 member 3	SLC22A3	0.0207
716	5-hydroxytryptamine 7 receptor	HTR7	0.0206
1820	Beta-nerve growth factor	NGF	0.0166
465	Calmodulin	CALM1	0.0163
6040	6-phosphogluconate dehydrogenase, decarboxylating	PGD	0.016
436	5-hydroxytryptamine 2B receptor	HTR2B	0.0157
341	5-hydroxytryptamine 3 receptor	HTR3A	0.0152
4146	Phosphatidylinositol 3-kinase regulatory subunit gamma	PIK3R3	0.0151
4145	Phosphatidylinositol 3-kinase regulatory subunit beta	PIK3R2	0.0151
3876	Aromatic-L-amino-acid decarboxylase	DDC	0.0139
220	Sodium channel protein type 5 subunit alpha	SCN5A	0.0134
1636	Trace amine-associated receptor 1	TAAR1	0.0134
1539	Oligopeptide transporter, small intestine isoform	SLC15A1	0.0133
1281	Phosphatidylinositol 3-kinase regulatory subunit alpha	PIK3R1	0.0125
4292	Acyl-[acyl-carrier-protein]--UDP-N-acetylglucosamine O-acyltransferase	lpxA	0.0124
3076	Antigen 85-C	fbpC	0.0122
777	Tumor necrosis factor	TNF	0.0121
3939	Amine oxidase [flavin-containing] B	MAOB	0.0116
6164	POU domain, class 5, transcription factor 1	POU5F1	0.0115
528	5-hydroxytryptamine 1E receptor	HTR1E	0.0115
847	Mu-type opioid receptor	OPRM1	0.0113
6138	Multidrug resistance protein 3	ABCB4	0.0113
20	Prostaglandin G/H synthase 1	PTGS1	0.011
124	Histamine H2 receptor	HRH2	0.0105
1732	ATP-binding cassette sub-family G member 2	ABCG2	0.0103
6022	UDP-glucuronosyltransferase 1-1	UGT1A1	0.0101
6106	Cytochrome P450 2C18	CYP2C18	0.0098
872	Gamma-aminobutyric-acid receptor subunit alpha-1	GABRA1	0.0095
6847	Lactase-phlorizin hydrolase	LCT	0.0093
6178	UDP-glucuronosyltransferase 2B7	UGT2B7	0.0092
467	Delta-type opioid receptor	OPRD1	0.0092
4115	Voltage-dependent L-type calcium channel subunit alpha-1D	CACNA1D	0.0092
478	Voltage-dependent L-type calcium channel subunit alpha-1C	CACNA1C	0.009
696	Kappa-type opioid receptor	OPRK1	0.0089
833	Organic cation/carnitine transporter 1	SLC22A4	0.0088
1374	Natriuretic peptides B	NPPB	0.0086
1827	Gap junction alpha-1 protein	GJA1	0.0086
1908	Vascular cell adhesion protein 1	VCAM1	0.0086
474	Acetylcholinesterase	ACHE	0.0084
1176	Mitogen-activated protein kinase 1	MAPK1	0.0083
6025	UDP-glucuronosyltransferase 1-4	UGT1A4	0.0082
4110	Voltage-dependent L-type calcium channel subunit beta-2	CACNB2	0.0081
6151	Monocarboxylate transporter 10	SLC16A10	0.0077
3947	Xanthine dehydrogenase/oxidase	XDH	0.0075
194	NADH dehydrogenase [ubiquinone] 1 subunit C2	NDUFC2	0.0071
4113	Voltage-dependent L-type calcium channel subunit alpha-1F	CACNA1F	0.0068
4111	Voltage-dependent L-type calcium channel subunit alpha-1S	CACNA1S	0.0067
183	Vascular endothelial growth factor A	VEGFA	0.0064
1898	Cytochrome P450 1B1	CYP1B1	0.0064
233	Potassium channel subfamily K member 2	KCNK2	0.0063
1656	CYP2B protein	CYP2B	0.0063
4114	Voltage-dependent L-type calcium channel subunit beta-3	CACNB3	0.006
4112	Voltage-dependent L-type calcium channel subunit beta-4	CACNB4	0.006
862	Multidrug resistance-associated protein 1	ABCC1	0.006
776	Bile salt export pump	ABCB11	0.0059
964	Voltage-dependent T-type calcium channel subunit alpha-1H	CACNA1H	0.0058
6432	Transporter	snf	0.0057
1632	Solute carrier organic anion transporter family member 2B1	SLCO2B1	0.0057
1490	Solute carrier organic anion transporter family member 1B1	SLCO1B1	0.0057
333	Voltage-dependent L-type calcium channel subunit beta-1	CACNB1	0.0055
1360	Sphingomyelin phosphodiesterase	SMPD1	0.0052
731	HIV-1 protease	HIV-1 protease	0.0052
6017	Cholesterol side-chain cleavage enzyme, mitochondrial	CYP11A1	0.005
6139	Solute carrier organic anion transporter family member 1A2	SLCO1A2	0.0049
734	D1 dopamine receptor-interacting protein calcyon	CALY	0.0049
6101	Dimethylaniline monooxygenase [N-oxide-forming] 3	FMO3	0.0049
158	Sodium channel protein type 1 subunit alpha	SCN1A	0.0047
6047	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A	PDE1A	0.0046
2112	Toll-like receptor 9	TLR9	0.0044
4120	NADPH--cytochrome P450 reductase	POR	0.0044
1735	Canalicular multispecific organic anion transporter 1	ABCC2	0.0043
5692	Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B	PDE1B	0.0043
4160	Voltage-dependent calcium channel subunit alpha-2/delta-2	CACNA2D2	0.0043
1729	Solute carrier family 22 member 6	SLC22A6	0.0041
360	Ribonucleoside-diphosphate reductase large subunit	RRM1	0.0039
3426	Glutamine synthetase	glnA	0.0037
3987	Glutamine synthetase	GLUL	0.0037
1561	Troponin C, slow skeletal and cardiac muscles	TNNC1	0.0035
762	Voltage-dependent calcium channel subunit alpha-2/delta-1	CACNA2D1	0.0035
6859	Protein S100-A4	S100A4	0.0035
4099	Gamma-aminobutyric-acid receptor subunit beta-3	GABRB3	0.0035
6104	Dimethylaniline monooxygenase [N-oxide-forming] 1	FMO1	0.0034
380	Cytochrome P450 17A1	CYP17A1	0.0034
6506	Stathmin-4	STMN4	0.0033
94	5-hydroxytryptamine 4 receptor	HTR4	0.0033
6182	Cytochrome P450 2J2	CYP2J2	0.0033
173	Toll-like receptor 7	TLR7	0.0033
198	Sodium channel protein type 10 subunit alpha	SCN10A	0.0033
817	DNA topoisomerase 2-alpha	TOP2A	0.0033
6018	UDP-glucuronosyltransferase 1-9	UGT1A9	0.0032
4199	Sphingosine 1-phosphate receptor Edg-8	S1PR5	0.0031
164	Histamine H4 receptor	HRH4	0.003
620	Bifunctional dihydrofolate reductase-thymidylate synthase	Not Available	0.003
565	Extracellular calcium-sensing receptor	CASR	0.0028
6031	Cytochrome P450 3A43	CYP3A43	0.0028
5251	Carbonyl reductase [NADPH] 1	CBR1	0.0027
1995	Sodium channel protein type 9 subunit alpha	SCN9A	0.0027
3804	Sodium channel protein type 4 subunit alpha	SCN4A	0.0026
6176	UDP-glucuronosyltransferase 1-3	UGT1A3	0.0025
813	Neuronal acetylcholine receptor subunit alpha-2	CHRNA2	0.0025
3811	Cytochrome P450 19A1	CYP19A1	0.0025
805	Cytochrome P450 11B1, mitochondrial	CYP11B1	0.0025
891	Dihydropteroate synthase	folP	0.0025
5359	Dihydropteroate synthase	folP	0.0025
7175	Dihydropteroate synthase	sulI	0.0025
161	Tubulin beta chain	TUBB	0.0024
312	Tubulin beta chain	TUB2	0.0024
750	Voltage-dependent calcium channel gamma-1 subunit	CACNG1	0.0024
631	3-hydroxy-3-methylglutaryl-coenzyme A reductase	HMGCR	0.0024
3387	3-hydroxy-3-methylglutaryl-coenzyme A reductase	mvaA	0.0024
6157	Solute carrier organic anion transporter family member 1B3	SLCO1B3	0.0024
6098	Potassium voltage-gated channel subfamily D member 2	KCND2	0.0023
6099	Potassium voltage-gated channel subfamily D member 3	KCND3	0.0023
385	Potassium-transporting ATPase alpha chain 1	ATP4A	0.0022
504	Mast/stem cell growth factor receptor	KIT	0.0022
952	Dipeptidyl peptidase 4	DPP4	0.0021
63	Malate dehydrogenase	mdh	0.0021
2329	Malate dehydrogenase	mdh	0.0021
3445	Malate dehydrogenase	mdh	0.0021
4420	Malate dehydrogenase	mdh	0.0021
4438	Malate dehydrogenase	mdh	0.0021
174	Sigma 1-type opioid receptor	SIGMAR1	0.002
365	Dihydrofolate reductase	DHFR	0.002
2381	Dihydrofolate reductase	DFR1	0.002
2833	Dihydrofolate reductase	Not Available	0.002
2931	Dihydrofolate reductase	folA	0.002
3544	Dihydrofolate reductase	folA	0.002
3682	Dihydrofolate reductase	folA	0.002
6642	Dihydrofolate reductase	folA	0.002
6756	Dihydrofolate reductase	dfrA	0.002
4203	Histamine N-methyltransferase	HNMT	0.0019
290	Prostaglandin G/H synthase 2	PTGS2	0.0019
2164	Multidrug resistance-associated protein 4	ABCC4	0.0019
871	Glucocorticoid receptor	NR3C1	0.0019
200	Carnitine O-palmitoyltransferase 2, mitochondrial	CPT2	0.0019
451	Carnitine O-palmitoyltransferase I, liver isoform	CPT1A	0.0019
15	Voltage-dependent T-type calcium channel subunit alpha-1I	CACNA1I	0.0018
893	[Citrate [pro-3S]-lyase] ligase	citC	0.0018
845	Pyruvate dehydrogenase [cytochrome]	poxB	0.0018
844	Epidermal growth factor receptor	EGFR	0.0018
327	Glutathione reductase	gor	0.0018
5110	Glutathione reductase	GR2	0.0018
1178	Adenosine A2a receptor	ADORA2A	0.0018
748	5'-AMP-activated protein kinase catalytic subunit alpha-1	PRKAA1	0.0018
650	Aldo-keto reductase family 1 member C3	AKR1C3	0.0017
535	Voltage-dependent T-type calcium channel subunit alpha-1G	CACNA1G	0.0017
392	Voltage-dependent P/Q-type calcium channel subunit alpha-1A	CACNA1A	0.0017
858	Potassium voltage-gated channel subfamily A member 1	KCNA1	0.0017
146	Androgen receptor	AR	0.0016
4209	ATP-sensitive inward rectifier potassium channel 8	KCNJ8	0.0016
4228	Keratin, type II cytoskeletal 7	KRT7	0.0016
1709	Canalicular multispecific organic anion transporter 2	ABCC3	0.0016
462	Intermediate conductance calcium-activated potassium channel protein 4	KCNN4	0.0016
6220	Aryl hydrocarbon receptor	AHR	0.0016
706	Glutamate [NMDA] receptor subunit 3A	GRIN3A	0.0016
610	Calcium-activated potassium channel subunit alpha 1	KCNMA1	0.0016
468	Cytochrome P450 4A11	CYP4A11	0.0016
1629	Transcription factor AP-1	JUN	0.0016
6180	UDP-glucuronosyltransferase 2B4	UGT2B4	0.0016
6142	Solute carrier family 22 member 8	SLC22A8	0.0016
982	Cocaine- and amphetamine-regulated transcript protein	CARTPT	0.0015
1618	High affinity nerve growth factor receptor	NTRK1	0.0015
238	Peroxisome proliferator-activated receptor gamma	PPARG	0.0015
4604	Liver carboxylesterase 1	CES1	0.0015
6023	Cytochrome P450 11B2, mitochondrial	CYP11B2	0.0015
1050	Bile salt sulfotransferase	SULT2A1	0.0014
6079	Neuronal acetylcholine receptor subunit alpha-3	CHRNA3	0.0014
3086	Plasmepsin-2	Not Available	0.0014
6100	BDNF/NT-3 growth factors receptor	NTRK2	0.0014
373	Transthyretin	TTR	0.0014
485	cGMP-inhibited 3',5'-cyclic phosphodiesterase A	PDE3A	0.0014
4148	Serine/threonine-protein kinase mTOR	MTOR	0.0014
738	Monocarboxylate transporter 1	SLC16A1	0.0014
208	DNA-directed RNA polymerase beta' chain	rpoC	0.0014
5774	DNA-directed RNA polymerase beta' chain	rpoC	0.0014
6143	Solute carrier family 22 member 7	SLC22A7	0.0013
698	B-Raf proto-oncogene serine/threonine-protein kinase	BRAF	0.0013
3404	Exotoxin A	eta	0.0013
17	Proto-oncogene tyrosine-protein kinase ABL1	ABL1	0.0013
950	Alpha platelet-derived growth factor receptor	PDGFRA	0.0013
73	Prostaglandin E2 receptor, EP1 subtype	PTGER1	0.0013
860	Nicotinamide N-methyltransferase	NNMT	0.0013
699	Nicotinic acid receptor 1	GPR109A	0.0013
928	Nicotinic acid receptor 2	GPR109B	0.0013
583	Nicotinate-nucleotide pyrophosphorylase [carboxylating]	QPRT	0.0013
2442	Nicotinate-nucleotide pyrophosphorylase [carboxylating]	nadC	0.0013
2459	Nicotinate-nucleotide pyrophosphorylase [carboxylating]	nadC	0.0013
458	Neuronal acetylcholine receptor subunit alpha-10	CHRNA10	0.0012
1010	Cytochrome P450 51A1	CYP51A1	0.0012
232	Corticosteroid-binding globulin	SERPINA6	0.0012
3856	Fibroblast growth factor receptor 3	FGFR3	0.0012
228	Beta platelet-derived growth factor receptor	PDGFRB	0.0012
5766	NAD-dependent deacetylase sirtuin-5	SIRT5	0.0012
6102	Arylamine N-acetyltransferase 2	NAT2	0.0012
6148	Multidrug resistance-associated protein 7	ABCC10	0.0012
473	L-lactate dehydrogenase A chain	LDHA	0.0011
464	Glutamate [NMDA] receptor subunit epsilon-2	GRIN2B	0.0011
6014	Cytochrome P450 2A13	CYP2A13	0.0011
707	72 kDa type IV collagenase	MMP2	0.0011
1086	Potassium voltage-gated channel subfamily KQT member 2	KCNQ2	0.0011
2290	ADP-ribosyl cyclase 2	BST1	0.001
614	Progesterone receptor	PGR	0.001
407	Vascular endothelial growth factor receptor 2	KDR	0.001
6181	UDP-glucuronosyltransferase 1-8	UGT1A8	0.001
4311	tRNA	TRDMT1	0.001
4325	tRNA	trmD	0.001
4328	tRNA	trmD	0.001
6080	Neuronal acetylcholine receptor subunit alpha-5	CHRNA5	0.001
6082	Neuronal acetylcholine receptor subunit beta-3	CHRNB3	0.001
948	Neuronal acetylcholine receptor subunit beta-2	CHRNB2	0.001
243	Ribosyldihydronicotinamide dehydrogenase [quinone]	NQO2	0.001
260	Cytochrome P450 51	ERG11	0.001
761	Cytochrome P450 51	ERG11	0.001
3163	Cytochrome P450 51	cyp51	0.001
144	Hemoglobin subunit alpha	HBA1	0.001
518	Peroxidase/catalase T	katG	0.001
6154	Multidrug and toxin extrusion protein 1	SLC47A1	0.0009
6081	Neuronal acetylcholine receptor subunit alpha-6	CHRNA6	0.0009
4097	Neuronal acetylcholine receptor subunit alpha-9	CHRNA9	0.0009
837	Glutamate [NMDA] receptor subunit epsilon-1	GRIN2A	0.0009
3126	Poly [ADP-ribose] polymerase 1	PARP1	0.0009
1064	DNA (cytosine-5)-methyltransferase 1	DNMT1	0.0009
563	Thyroid peroxidase	TPO	0.0009
147	Aldehyde dehydrogenase, mitochondrial	ALDH2	0.0009
65	Matrix metalloproteinase-9	Not Available	0.0009
26	Vascular endothelial growth factor receptor 3	FLT4	0.0009
295	Carbonic anhydrase 1	CA1	0.0009
741	Potassium voltage-gated channel subfamily KQT member 1	KCNQ1	0.0009
4122	Histone deacetylase 2	HDAC2	0.0009
16	Adenosine A1 receptor	ADORA1	0.0009
241	Calcium-transporting ATPase type 2C member 1	ATP2C1	0.0009
32	Vascular endothelial growth factor receptor 1	FLT1	0.0009
634	Squalene monooxygenase	SQLE	0.0009
7196	Squalene monooxygenase	ERG1	0.0009
204	cGMP-specific 3',5'-cyclic phosphodiesterase	PDE5A	0.0009
6078	Neuronal acetylcholine receptor subunit beta-4	CHRNB4	0.0009
1262	Corticotropin-lipotropin	POMC	0.0008
1341	Histamine H3 receptor	HRH3	0.0008
3932	Glutathione S-transferase A2	GSTA2	0.0008
537	ATP synthase delta chain, mitochondrial	ATP5D	0.0008
1192	Sulfotransferase 1A1	SULT1A1	0.0008
778	Cysteinyl leukotriene receptor 1	CYSLTR1	0.0008
522	26S proteasome non-ATPase regulatory subunit 2	PSMD2	0.0008
515	26S proteasome non-ATPase regulatory subunit 1	PSMD1	0.0008
1457	Long-chain-fatty-acid--CoA ligase 4	ACSL4	0.0008
165	FL cytokine receptor	FLT3	0.0008
244	Angiotensin-converting enzyme	ACE	0.0008
559	NADH-ubiquinone oxidoreductase chain 1	MT-ND1	0.0008
6126	Carbonic anhydrase 7	CA7	0.0008
6212	Tubulin gamma-1 chain	TUBG1	0.0008
6210	Tubulin delta chain	TUBD1	0.0008
6211	Tubulin epsilon chain	TUBE1	0.0008
2180	3-phosphoinositide-dependent protein kinase 1	PDPK1	0.0008
4177	Proto-oncogene tyrosine-protein kinase receptor ret	RET	0.0008
482	Glycine receptor subunit alpha-1	GLRA1	0.0008
500	Monocarboxylate transporter 4	SLC16A3	0.0008
70	Type-1 angiotensin II receptor	AGTR1	0.0008
1974	Oligopeptide transporter, kidney isoform	SLC15A2	0.0008
6137	Multidrug resistance-associated protein 6	ABCC6	0.0008
866	Large neutral amino acids transporter small subunit 2	SLC7A8	0.0007
606	Cytochrome P450 27, mitochondrial	CYP27A1	0.0007
541	cAMP-specific 3',5'-cyclic phosphodiesterase 4B	PDE4B	0.0007
3854	Basic fibroblast growth factor receptor 1	FGFR1	0.0007
122	P2Y purinoceptor 12	P2RY12	0.0007
6136	Multidrug resistance-associated protein 5	ABCC5	0.0007
581	Cytochrome P450 2R1	CYP2R1	0.0007
580	Gamma-aminobutyric-acid receptor subunit alpha-3	GABRA3	0.0007
423	Gamma-aminobutyric-acid receptor subunit alpha-2	GABRA2	0.0007
439	Glutamate [NMDA] receptor subunit epsilon-4	GRIN2D	0.0007
5878	Alpha-7 nicotinic cholinergic receptor subunit	CHRFAM7A	0.0007
6038	Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma	PDE6H	0.0007
505	Glutamate [NMDA] receptor subunit epsilon-3	GRIN2C	0.0007
245	Large neutral amino acids transporter small subunit 1	SLC7A5	0.0007
4773	Deoxycytidine kinase	DCK	0.0007
2222	Equilibrative nucleoside transporter 1	SLC29A1	0.0007
1992	Vitamin D-binding protein	GC	0.0007
319	Opioid receptor, sigma 1	OPRS1	0.0007
368	Enoyl-[acyl-carrier-protein] reductase [NADH]	inhA	0.0007
3228	Enoyl-[acyl-carrier-protein] reductase [NADH]	fabI	0.0007
3678	Enoyl-[acyl-carrier-protein] reductase [NADH]	fabI	0.0007
6856	Enoyl-[acyl-carrier-protein] reductase [NADH]	fabI	0.0007
215	Sodium channel protein type 11 subunit alpha	SCN11A	0.0007
7	Nitric oxide synthase, inducible	NOS2	0.0007
6037	Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gamma	PDE6G	0.0007
737	Mineralocorticoid receptor	NR3C2	0.0006
401	Glutamate [NMDA] receptor subunit zeta-1	GRIN1	0.0006
592	Carbonic anhydrase 4	CA4	0.0006
976	Platelet glycoprotein IX	GP9	0.0006
4103	Proteasome subunit beta type 2	PSMB2	0.0006
4102	Proteasome subunit beta type 5	PSMB5	0.0006
4101	Proteasome subunit beta type 1	PSMB1	0.0006
1630	Integrin beta-2	ITGB2	0.0006
2450	Tyrosine-protein kinase ITK/TSK	ITK	0.0006
3970	Voltage-dependent N-type calcium channel subunit alpha-1B	CACNA1B	0.0006
2216	Fibroblast growth factor receptor 4	FGFR4	0.0006
4095	Neuronal acetylcholine receptor subunit alpha-7	CHRNA7	0.0006
947	Neuronal acetylcholine receptor subunit alpha-4	CHRNA4	0.0006
806	Sodium/potassium-transporting ATPase alpha-1 chain	ATP1A1	0.0006
814	Ryanodine receptor 1	RYR1	0.0006
511	5-hydroxytryptamine 1F receptor	HTR1F	0.0006
6141	Sodium/bile acid cotransporter	SLC10A1	0.0006
6146	High affinity copper uptake protein 1	SLC31A1	0.0006
4100	Gamma-aminobutyric-acid receptor subunit beta-2	GABRB2	0.0006
1757	Myeloperoxidase	MPO	0.0006
2449	Tubulin alpha-3 chain	TUBA1A	0.0006
6046	Voltage-gated calcium channel beta 1 subunit splice variant CavB1d	CACNB1	0.0006
705	Glutamate receptor 1	GRIA1	0.0006
6048	Troponin C, skeletal muscle	TNNC2	0.0005
543	Penicillin-binding protein 1B	mrcB	0.0005
6186	Penicillin-binding protein 1B	ponB	0.0005
6822	Penicillin-binding protein 1b	pbp1b	0.0005
6844	Penicillin-binding protein 1b	pbp1b	0.0005
645	Penicillin-binding protein 1A	mrcA	0.0005
5805	Penicillin-binding protein 1A	ponA	0.0005
6185	Penicillin-binding protein 1A	mrcA	0.0005
6799	Penicillin-binding protein 1A	pbpA	0.0005
268	Adenosine A2b receptor	ADORA2B	0.0005
159	Penicillin-binding protein 2B	penA	0.0005
6121	Penicillin-binding protein 2B	penA	0.0005
6044	Serum paraoxonase/lactonase 3	PON3	0.0005
1024	Solute carrier family 22 member 11	SLC22A11	0.0005
6045	Voltage-dependent calcium channel subunit alpha-2/delta-3	CACNA2D3	0.0005
856	Vitamin D3 receptor	VDR	0.0005
1284	Nuclear receptor subfamily 1 group I member 2	NR1I2	0.0005
572	Integrin alpha-L	ITGAL	0.0005
904	Glutathione S-transferase P	GSTP1	0.0005
3868	Calcineurin subunit B isoform 2	PPP3R2	0.0005
357	Carbonic anhydrase 2	CA2	0.0005
421	Calcium signal-modulating cyclophilin ligand	CAMLG	0.0005
1864	RET proto-oncogene	RET	0.0005
1950	Epithelial discoidin domain-containing receptor 1	DDR1	0.0005
6094	BCR/ABL fusion protein isoform X9	BCR/ABL fusion	0.0005
6170	ATP-binding cassette sub-family A member 3	ABCA3	0.0005
6824	Tyrosine-protein kinase Lyn	LYN	0.0005
1275	Estrogen sulfotransferase	SULT1E1	0.0004
3802	Sodium channel protein type 2 subunit alpha	SCN2A	0.0004
136	Estrogen receptor	ESR1	0.0004
153	Dopamine beta-hydroxylase	DBH	0.0004
760	Fibroblast growth factor 1	FGF1	0.0004
6931	Calcium-activated potassium channel subunit beta-1	KCNMB1	0.0004
6933	Calcium-activated potassium channel subunit beta-4	KCNMB4	0.0004
6932	Calcium-activated potassium channel subunit beta-3	KCNMB3	0.0004
6934	Small conductance calcium-activated potassium channel protein 1	KCNN1	0.0004
6935	Small conductance calcium-activated potassium channel protein 2	KCNN2	0.0004
6936	Small conductance calcium-activated potassium channel protein 3	KCNN3	0.0004
1768	Guanine nucleotide-binding protein G(I)/G(S)/G(O) gamma-2 subunit	GNG2	0.0004
1581	G protein-activated inward rectifier potassium channel 2	KCNJ6	0.0004
1571	G protein-activated inward rectifier potassium channel 1	KCNJ3	0.0004
1268	Neuropeptide S receptor	NPSR1	0.0004
5787	Angiopoietin-1 receptor	TEK	0.0004
230	ATP-binding cassette transporter sub-family C member 8	ABCC8	0.0004
823	Fibroblast growth factor receptor 2	FGFR2	0.0004
291	Nitric-oxide synthase, endothelial	NOS3	0.0004
5934	Cytochrome P450 26A1	CYP26A1	0.0004
751	Potassium channel subfamily K member 6	KCNK6	0.0004
6177	UDP-glucuronosyltransferase 1-10	UGT1A10	0.0004
6172	ATP-binding cassette sub-family B member 8, mitochondrial	ABCB8	0.0004
6073	Potassium channel subfamily K member 9	KCNK9	0.0004
6072	Potassium channel subfamily K member 3	KCNK3	0.0004
3937	Fatty-acid amide hydrolase	FAAH	0.0004
5463	Calcium-activated potassium channel subunit beta 2	KCNMB2	0.0004
172	Potassium channel subfamily K member 1	KCNK1	0.0004
40	RAF proto-oncogene serine/threonine-protein kinase	RAF1	0.0004
1524	Peptidyl-prolyl cis-trans isomerase A	PPIA	0.0004
6700	Peptidyl-prolyl cis-trans isomerase A	ppiA	0.0004
1971	cAMP-specific 3',5'-cyclic phosphodiesterase 4A	PDE4A	0.0004
951	Macrophage colony-stimulating factor 1 receptor	CSF1R	0.0004
84	Nuclear receptor 0B1	NR0B1	0.0004
337	NADH dehydrogenase [ubiquinone] iron-sulfur protein 7, mitochondrial	NDUFS7	0.0004
214	NADH dehydrogenase [ubiquinone] iron-sulfur protein 3, mitochondrial	NDUFS3	0.0004
803	NADH dehydrogenase [ubiquinone] iron-sulfur protein 2, mitochondrial	NDUFS2	0.0004
3957	Adenosine deaminase	ADA	0.0004
6168	Solute carrier family 22 member 16	SLC22A16	0.0003
937	Proto-oncogene tyrosine-protein kinase LCK	LCK	0.0003
6861	Alcohol dehydrogenase [NADP+]	AKR1A1	0.0003
6140	Ileal sodium/bile acid cotransporter	SLC10A2	0.0003
469	Annexin A1	ANXA1	0.0003
591	Glutamate [NMDA] receptor subunit 3B	GRIN3B	0.0003
6091	Gamma-aminobutyric acid receptor subunit theta	GABRQ	0.0003
2207	Rhodopsin	RHO	0.0003
6086	Gamma-aminobutyric acid receptor subunit gamma-2	GABRG2	0.0003
6090	Gamma-aminobutyric acid receptor subunit pi	GABRP	0.0003
6092	Gamma-aminobutyric acid receptor subunit rho-2	GABRR2	0.0003
6088	Gamma-aminobutyric acid receptor subunit gamma-3	GABRG3	0.0003
6115	Gamma-aminobutyric acid receptor subunit rho-3	GABRR3	0.0003
6087	Gamma-aminobutyric acid receptor subunit gamma-1	GABRG1	0.0003
6093	Gamma-aminobutyric acid receptor subunit delta	GABRD	0.0003
6089	Gamma-aminobutyric acid receptor subunit epsilon	GABRE	0.0003
142	Gamma-aminobutyric-acid receptor subunit rho-1	GABRR1	0.0003
4098	Gamma-aminobutyric-acid receptor subunit beta-1	GABRB1	0.0003
933	Proto-oncogene tyrosine-protein kinase Src	SRC	0.0003
841	Gamma-aminobutyric-acid receptor subunit alpha-6	GABRA6	0.0003
530	Gamma-aminobutyric-acid receptor subunit alpha-4	GABRA4	0.0003
523	Gamma-aminobutyric-acid receptor subunit alpha-5	GABRA5	0.0002
2157	NAD(P)H dehydrogenase [quinone] 1	NQO1	0.0002
869	Estrogen receptor beta	ESR2	0.0002
76	Nitric-oxide synthase, brain	NOS1	0.0002
781	ATP-sensitive inward rectifier potassium channel 11	KCNJ11	0.0002

(*) Categorization taken from DrugBank: therapeutic category or general category of a drug (i.e. anti-convulsant, antibacterial, etc.)

DB00598 - Labetalol

Targets

Enzymes

Predictions