DT-Web

DB00797 - Tolazoline


Identification
Name Tolazoline
Accession Number DB00797 (APRD00170)
Type small molecule
Description A vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 160.2157
Groups approved
Monoisotopic Weight 160.100048394
Pharmacology
Indication For the treatment of pulmonary artery anomalies
Mechanism of action Vasodilation by means of a direct effect on peripheral vascular smooth muscle and indirect effects produced, in part, by release of endogenous histamine; tolazoline has moderate alpha-adrenergic blocking activity and has histamine agonist activity. Tolazoline usually reduces pulmonary arterial pressure and vascular resistance.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Cimetidine Anticipated loss of efficacy of tolazoline
Ranitidine Anticipated loss of efficacy of tolazoline
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Food Interactions Not Available

Targets


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
  • Teskin O, Uydes-Dogan BS, Enc Y, Alp FI, Kaleli D, Keser S, Iyigun T, Bilgen F, Dagsali S, Ozdemir O: Comparative effects of tolazoline and nitroprusside on human isolated radial artery. Ann Thorac Surg. 2006 Jan;81(1):125-31. - Pubmed
  • Song W, Zhang Y, Xia L, Liu G: [Effects of some mexiletine derivatives on alpha 1-adrenoceptors] Yao Xue Xue Bao. 1998;33(2):102-5. - Pubmed
DTHybrid score 0.3803
Alpha-2A adrenergic receptor
Name Alpha-2A adrenergic receptor
Gene Name ADRA2A
Pharmacological action unknown
Actions antagonist
References
  • Song W, Zhang Y, Xia L, Liu G: [Effects of some mexiletine derivatives on alpha 1-adrenoceptors] Yao Xue Xue Bao. 1998;33(2):102-5. - Pubmed
DTHybrid score 0.335
Histamine H1 receptor
Name Histamine H1 receptor
Gene Name HRH1
Pharmacological action unknown
Actions agonist
References
  • Roll C, Hanssler L: [Interaction of tolazoline and cimetidine in persistent fetal circulation of the newborn infant] Monatsschr Kinderheilkd. 1993 Apr;141(4):297-9. - Pubmed
DTHybrid score 0.5195

Predictions


Id Partner name Gene Name Score
4119 Cytochrome P450 2D6 CYP2D6 0.1242
632 Alpha-1B adrenergic receptor ADRA1B 0.1145
4512 Cytochrome P450 3A4 CYP3A4 0.0972
502 5-hydroxytryptamine 2A receptor HTR2A 0.0911
629 Alpha-2B adrenergic receptor ADRA2B 0.0868
378 Alpha-2C adrenergic receptor ADRA2C 0.0855
23 D(1A) dopamine receptor DRD1 0.0784
831 D(2) dopamine receptor DRD2 0.0737
789 Alpha-1D adrenergic receptor ADRA1D 0.0695
4200 Cytochrome P450 1A2 CYP1A2 0.0666
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0651
320 5-hydroxytryptamine 1A receptor HTR1A 0.0592
590 5-hydroxytryptamine 2C receptor HTR2C 0.0576
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0571
1588 Multidrug resistance protein 1 ABCB1 0.0532
713 Sodium-dependent dopamine transporter SLC6A3 0.046
824 Sodium-dependent serotonin transporter SLC6A4 0.0431
617 Muscarinic acetylcholine receptor M2 CHRM2 0.04
432 D(4) dopamine receptor DRD4 0.0393
766 Beta-2 adrenergic receptor ADRB2 0.0392
638 D(3) dopamine receptor DRD3 0.0367
131 Synaptic vesicular amine transporter SLC18A2 0.0361
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0357
725 5-hydroxytryptamine 1D receptor HTR1D 0.0357
193 Beta-1 adrenergic receptor ADRB1 0.0348
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0348
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0347
163 D(1B) dopamine receptor DRD5 0.0342
4757 Cytochrome P450 2C9 CYP2C9 0.0339
6016 Cytochrome P450 2C19 CYP2C19 0.0322
885 5-hydroxytryptamine 1B receptor HTR1B 0.0311
716 5-hydroxytryptamine 7 receptor HTR7 0.0297
6030 Cytochrome P450 2B6 CYP2B6 0.027
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0249
4118 Cytochrome P450 3A5 CYP3A5 0.0233
6013 Cytochrome P450 2E1 CYP2E1 0.0228
3941 Amine oxidase [flavin-containing] A MAOA 0.0226
436 5-hydroxytryptamine 2B receptor HTR2B 0.0224
6145 Solute carrier family 22 member 1 SLC22A1 0.0223
1256 5-hydroxytryptamine 6 receptor HTR6 0.0194
6107 Cytochrome P450 3A7 CYP3A7 0.0179
1341 Histamine H3 receptor HRH3 0.0175
516 Neurotensin receptor type 2 NTSR2 0.0168
6144 Solute carrier family 22 member 2 SLC22A2 0.0162
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0161
118 Organic cation/carnitine transporter 2 SLC22A5 0.0148
6147 Solute carrier family 22 member 3 SLC22A3 0.0146
124 Histamine H2 receptor HRH2 0.0137
341 5-hydroxytryptamine 3 receptor HTR3A 0.0134
3923 Cholinesterase BCHE 0.0131
4924 Cytochrome P450 2C8 CYP2C8 0.0122
1656 CYP2B protein CYP2B 0.0122
528 5-hydroxytryptamine 1E receptor HTR1E 0.012
465 Calmodulin CALM1 0.0111
6024 Cytochrome P450 1A1 CYP1A1 0.0109
828 Phenylalanine-4-hydroxylase PAH 0.0104
3109 Phenylalanine-4-hydroxylase phhA 0.0104
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0101
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.01
587 Serum albumin ALB 0.0098
1517 Beta-3 adrenergic receptor ADRB3 0.0095
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0086
1275 Estrogen sulfotransferase SULT1E1 0.0086
3426 Glutamine synthetase glnA 0.0084
3987 Glutamine synthetase GLUL 0.0084
833 Organic cation/carnitine transporter 1 SLC22A4 0.0083
3810 Catechol O-methyltransferase COMT 0.0083
3939 Amine oxidase [flavin-containing] B MAOB 0.0083
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0078
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0078
6154 Multidrug and toxin extrusion protein 1 SLC47A1 0.0076
6070 Nischarin NISCH 0.0075
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0074
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0071
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0069
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.0068
4120 NADPH--cytochrome P450 reductase POR 0.0067
1636 Trace amine-associated receptor 1 TAAR1 0.0066
6020 Aldehyde oxidase AOX1 0.0062
5718 Cytochrome P450 2A6 CYP2A6 0.0056
696 Kappa-type opioid receptor OPRK1 0.0052
6182 Cytochrome P450 2J2 CYP2J2 0.005
6097 Protein S100-A2 S100A2 0.005
1810 Protein S100-A1 S100A1 0.005
164 Histamine H4 receptor HRH4 0.0048
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0045
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0045
1729 Solute carrier family 22 member 6 SLC22A6 0.0043
6138 Multidrug resistance protein 3 ABCB4 0.0043
1048 Protein S100-A13 S100A13 0.0043
2226 Protein S100-A12 S100A12 0.0043
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0042
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0042
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0041
6106 Cytochrome P450 2C18 CYP2C18 0.0041
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.004
2132 Protein S100-B S100B 0.004
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0039
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0037
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0035
6432 Transporter snf 0.0035
6859 Protein S100-A4 S100A4 0.0035
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0035
6217 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B PDE8B 0.0035
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0034
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0034
20 Prostaglandin G/H synthase 1 PTGS1 0.0033
474 Acetylcholinesterase ACHE 0.0032
233 Potassium channel subfamily K member 2 KCNK2 0.0031
6216 High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A PDE8A 0.003
691 cAMP-specific 3',5'-cyclic phosphodiesterase 7B PDE7B 0.0029
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0029
6151 Monocarboxylate transporter 10 SLC16A10 0.0028
3947 Xanthine dehydrogenase/oxidase XDH 0.0028
1618 High affinity nerve growth factor receptor NTRK1 0.0027
779 High-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A PDE7A 0.0026
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0026
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0026
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0026
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0026
439 Glutamate [NMDA] receptor subunit epsilon-4 GRIN2D 0.0026
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0024
6157 Solute carrier organic anion transporter family member 1B3 SLCO1B3 0.0024
1360 Sphingomyelin phosphodiesterase SMPD1 0.0024
4109 cAMP-specific 3',5'-cyclic phosphodiesterase 4C PDE4C 0.0024
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0024
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0024
591 Glutamate [NMDA] receptor subunit 3B GRIN3B 0.0023
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0023
401 Glutamate [NMDA] receptor subunit zeta-1 GRIN1 0.0023
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0021
6040 6-phosphogluconate dehydrogenase, decarboxylating PGD 0.0021
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0021
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0021
776 Bile salt export pump ABCB11 0.002
1971 cAMP-specific 3',5'-cyclic phosphodiesterase 4A PDE4A 0.002
198 Sodium channel protein type 10 subunit alpha SCN10A 0.002
2358 cAMP-specific 3',5'-cyclic phosphodiesterase 4D PDE4D 0.0019
4203 Histamine N-methyltransferase HNMT 0.0019
1374 Natriuretic peptides B NPPB 0.0019
1827 Gap junction alpha-1 protein GJA1 0.0019
1908 Vascular cell adhesion protein 1 VCAM1 0.0019
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0019
541 cAMP-specific 3',5'-cyclic phosphodiesterase 4B PDE4B 0.0018
467 Delta-type opioid receptor OPRD1 0.0017
194 NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2 0.0016
183 Vascular endothelial growth factor A VEGFA 0.0014
1898 Cytochrome P450 1B1 CYP1B1 0.0014
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0011
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0011
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0011
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0008
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