DT-Web

DB00723 - Methoxamine


Identification
Name Methoxamine
Accession Number DB00723 (APRD00062)
Type small molecule
Description An alpha-adrenergic agonist that causes prolonged peripheral vasoconstriction. It has little if any direct effect on the central nervous system. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 211.2576
Groups approved
Monoisotopic Weight 211.120843415
Pharmacology
Indication Indicated for the treatment and management of hypotension.
Mechanism of action Methoxamine acts through peripheral vasoconstriction by acting as a pure alpha-1 adrenergic receptor agonist, consequently increasing systemic blood pressure (both systolic and diastolic).
Absorption Not Available
Protein binding Low
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of methoxamine.
Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of methoxamine.
Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of methoxamine.
Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of methoxamine.
Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of methoxamine.
Guanethidine Methoxamine may decrease the effect of guanethidine.
Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of methoxamine.
Isocarboxazid Increased arterial pressure
Linezolid Possible increase of arterial pressure
Methyldopa Increased arterial pressure
Midodrine Increased arterial pressure
Moclobemide Moclobemide increases the sympathomimetic effect of methoxamine.
Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of methoxamine.
Phenelzine Increased arterial pressure
Rasagiline Increased arterial pressure
Reserpine Increased arterial pressure
Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha1-agonist, Methoxamine. Concomitant therapy should be avoided.
Trimipramine Trimipramine may increase the vasopressor effect of the alpha1-agonist, Methoxamine. Avoid combination if possible. Monitor sympathetic response to therapy if used concomitantly.
Food Interactions Not Available

Targets


Alpha-1A adrenergic receptor
Name Alpha-1A adrenergic receptor
Gene Name ADRA1A
Pharmacological action yes
Actions agonist
References
  • Satoh M, Kojima C, Kokubu N, Takayanagi I: Alpha 1-adrenoceptor subtypes mediating the regulation and modulation of Ca2+ sensitization in rabbit thoracic aorta. Eur J Pharmacol. 1994 Nov 24;265(3):133-9. - Pubmed
  • Suzuki E, Tsujimoto G, Tamura K, Hashimoto K: Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role. Mol Pharmacol. 1990 Nov;38(5):725-36. - Pubmed
  • Piascik MT, Sparks MS, Pruitt TA, Soltis EE: Evidence for a complex interaction between the subtypes of the alpha 1-adrenoceptor. Eur J Pharmacol. 1991 Jul 9;199(3):279-89. - Pubmed
  • Sattar MA, Johns EJ: Evidence for an alpha 1-adrenoceptor subtype mediating adrenergic vasoconstriction in Wistar normotensive and stroke-prone spontaneously hypertensive rat kidney. J Cardiovasc Pharmacol. 1994 Feb;23(2):232-9. - Pubmed
  • Hoang TV, Choe EU, Burgess RS, Cork RC, Flint LM, Ferrara JJ: Characterization of alpha-adrenoceptor activity in the preterm piglet mesentery. J Pediatr Surg. 1996 Dec;31(12):1659-62. - Pubmed
DTHybrid score 0.374
Alpha-1B adrenergic receptor
Name Alpha-1B adrenergic receptor
Gene Name ADRA1B
Pharmacological action unknown
Actions agonist
References
  • Tsujimoto G, Tsujimoto A, Suzuki E, Hashimoto K: Glycogen phosphorylase activation by two different alpha 1-adrenergic receptor subtypes: methoxamine selectively stimulates a putative alpha 1-adrenergic receptor subtype (alpha 1a) that couples with Ca2+ influx. Mol Pharmacol. 1989 Jul;36(1):166-76. - Pubmed
  • Simpson P: Stimulation of hypertrophy of cultured neonatal rat heart cells through an alpha 1-adrenergic receptor and induction of beating through an alpha 1- and beta 1-adrenergic receptor interaction. Evidence for independent regulation of growth and beating. Circ Res. 1985 Jun;56(6):884-94. - Pubmed
  • Oleksa LM, Hool LC, Harvey RD: Alpha 1-adrenergic inhibition of the beta-adrenergically activated Cl- current in guinea pig ventricular myocytes. Circ Res. 1996 Jun;78(6):1090-9. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Waugh DJ, Gaivin RJ, Zuscik MJ, Gonzalez-Cabrera P, Ross SA, Yun J, Perez DM: Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists. J Biol Chem. 2001 Jul 6;276(27):25366-71. Epub 2001 Apr 30. - Pubmed
DTHybrid score 0.2636

Predictions


Id Partner name Gene Name Score
789 Alpha-1D adrenergic receptor ADRA1D 0.1193
318 Alpha-2A adrenergic receptor ADRA2A 0.1126
4119 Cytochrome P450 2D6 CYP2D6 0.0685
831 D(2) dopamine receptor DRD2 0.0645
502 5-hydroxytryptamine 2A receptor HTR2A 0.0643
23 D(1A) dopamine receptor DRD1 0.0639
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0576
4512 Cytochrome P450 3A4 CYP3A4 0.0548
629 Alpha-2B adrenergic receptor ADRA2B 0.0481
320 5-hydroxytryptamine 1A receptor HTR1A 0.0428
1588 Multidrug resistance protein 1 ABCB1 0.042
378 Alpha-2C adrenergic receptor ADRA2C 0.0401
713 Sodium-dependent dopamine transporter SLC6A3 0.0397
492 Histamine H1 receptor HRH1 0.0385
4200 Cytochrome P450 1A2 CYP1A2 0.0355
590 5-hydroxytryptamine 2C receptor HTR2C 0.035
766 Beta-2 adrenergic receptor ADRB2 0.0325
193 Beta-1 adrenergic receptor ADRB1 0.032
131 Synaptic vesicular amine transporter SLC18A2 0.0294
432 D(4) dopamine receptor DRD4 0.0279
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0276
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0258
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0241
274 Muscarinic acetylcholine receptor M5 CHRM5 0.024
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0233
6145 Solute carrier family 22 member 1 SLC22A1 0.0219
725 5-hydroxytryptamine 1D receptor HTR1D 0.021
638 D(3) dopamine receptor DRD3 0.021
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0208
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0206
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0206
6016 Cytochrome P450 2C19 CYP2C19 0.0205
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0204
824 Sodium-dependent serotonin transporter SLC6A4 0.0193
1256 5-hydroxytryptamine 6 receptor HTR6 0.0173
163 D(1B) dopamine receptor DRD5 0.0167
4757 Cytochrome P450 2C9 CYP2C9 0.0162
885 5-hydroxytryptamine 1B receptor HTR1B 0.0162
3941 Amine oxidase [flavin-containing] A MAOA 0.016
4118 Cytochrome P450 3A5 CYP3A5 0.0151
716 5-hydroxytryptamine 7 receptor HTR7 0.015
587 Serum albumin ALB 0.014
6013 Cytochrome P450 2E1 CYP2E1 0.0131
828 Phenylalanine-4-hydroxylase PAH 0.012
3109 Phenylalanine-4-hydroxylase phhA 0.012
6138 Multidrug resistance protein 3 ABCB4 0.0113
6144 Solute carrier family 22 member 2 SLC22A2 0.0106
6030 Cytochrome P450 2B6 CYP2B6 0.0104
1636 Trace amine-associated receptor 1 TAAR1 0.0102
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0099
528 5-hydroxytryptamine 1E receptor HTR1E 0.0097
6107 Cytochrome P450 3A7 CYP3A7 0.0095
3923 Cholinesterase BCHE 0.0091
6147 Solute carrier family 22 member 3 SLC22A3 0.009
1517 Beta-3 adrenergic receptor ADRB3 0.0082
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0077
436 5-hydroxytryptamine 2B receptor HTR2B 0.0077
341 5-hydroxytryptamine 3 receptor HTR3A 0.0077
465 Calmodulin CALM1 0.007
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0064
118 Organic cation/carnitine transporter 2 SLC22A5 0.0057
4924 Cytochrome P450 2C8 CYP2C8 0.0051
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0049
124 Histamine H2 receptor HRH2 0.0049
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0046
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0046
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0046
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0045
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0044
6024 Cytochrome P450 1A1 CYP1A1 0.0044
1656 CYP2B protein CYP2B 0.0044
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0038
3426 Glutamine synthetase glnA 0.0037
3987 Glutamine synthetase GLUL 0.0037
233 Potassium channel subfamily K member 2 KCNK2 0.0036
6859 Protein S100-A4 S100A4 0.0035
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0034
6151 Monocarboxylate transporter 10 SLC16A10 0.0033
474 Acetylcholinesterase ACHE 0.0032
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0032
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0031
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0031
4120 NADPH--cytochrome P450 reductase POR 0.003
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0029
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0028
3947 Xanthine dehydrogenase/oxidase XDH 0.0028
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0028
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0028
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0028
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0027
776 Bile salt export pump ABCB11 0.0026
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0024
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0024
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0022
3939 Amine oxidase [flavin-containing] B MAOB 0.0021
164 Histamine H4 receptor HRH4 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
6432 Transporter snf 0.0018
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0017
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0017
194 NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2 0.0016
5718 Cytochrome P450 2A6 CYP2A6 0.0015
183 Vascular endothelial growth factor A VEGFA 0.0014
20 Prostaglandin G/H synthase 1 PTGS1 0.0014
6106 Cytochrome P450 2C18 CYP2C18 0.0012
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
833 Organic cation/carnitine transporter 1 SLC22A4 0.0012
1898 Cytochrome P450 1B1 CYP1B1 0.0011
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0011
1618 High affinity nerve growth factor receptor NTRK1 0.0008
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0008
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0006
467 Delta-type opioid receptor OPRD1 0.0005
696 Kappa-type opioid receptor OPRK1 0.0005
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