DT-Web

DB01365 - Mephentermine


Identification
Name Mephentermine
Accession Number DB01365
Type small molecule
Description A sympathomimetic agent with mainly indirect effects on adrenergic receptors. It is used to maintain blood pressure in hypotensive states, for example, following spinal anesthesia. Although the central stimulant effects of mephentermine are much less than those of amphetamine, its use may lead to amphetamine-type dependence. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1248)
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 163.2594
Groups approved
Monoisotopic Weight 163.136099549
Pharmacology
Indication Used to maintain blood pressure in hypotensive states.
Mechanism of action Mephentermine is an alpha adrenergic receptor agonist, but also acts indirectly by releasing endogenous norepinephrine. Cardiac output and systolic and diastolic pressures are usually increased. A change in heart rate is variable, depending on the degree of vagal tone. Sometimes the net vascular effect may be vasodilation. Large doses may depress the myocardium or produce central nervous system (CNS) effects.
Absorption Not Available
Protein binding Not Available
Biotransformation Hepatic, by N-demethylation and then p-hydroxylation.
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 mephentermine.
Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of mephentermine.
Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of mephentermine.
Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of mephentermine.
Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of mephentermine.
Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of mephentermine.
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 mephentermine.
Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of mephentermine.
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, Mephentermine. Concomitant therapy should be avoided.
Trimipramine Trimipramine may increase the vasopressor effect of the alpha1-agonist, Mephentermine. 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
  • 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
  • Ahlquist RP: Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor. Am Heart J. 1976 Nov;92(5):661-4. - Pubmed
DTHybrid score 0.2628

Predictions


Id Partner name Gene Name Score
318 Alpha-2A adrenergic receptor ADRA2A 0.0789
632 Alpha-1B adrenergic receptor ADRA1B 0.0772
789 Alpha-1D adrenergic receptor ADRA1D 0.0463
4119 Cytochrome P450 2D6 CYP2D6 0.0382
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0353
831 D(2) dopamine receptor DRD2 0.0351
502 5-hydroxytryptamine 2A receptor HTR2A 0.0333
23 D(1A) dopamine receptor DRD1 0.0291
4512 Cytochrome P450 3A4 CYP3A4 0.0288
492 Histamine H1 receptor HRH1 0.0245
131 Synaptic vesicular amine transporter SLC18A2 0.0243
1588 Multidrug resistance protein 1 ABCB1 0.0237
766 Beta-2 adrenergic receptor ADRB2 0.0217
320 5-hydroxytryptamine 1A receptor HTR1A 0.0208
193 Beta-1 adrenergic receptor ADRB1 0.0199
629 Alpha-2B adrenergic receptor ADRA2B 0.0199
4200 Cytochrome P450 1A2 CYP1A2 0.0178
378 Alpha-2C adrenergic receptor ADRA2C 0.0175
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0164
824 Sodium-dependent serotonin transporter SLC6A4 0.0149
713 Sodium-dependent dopamine transporter SLC6A3 0.0146
590 5-hydroxytryptamine 2C receptor HTR2C 0.0146
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0133
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0124
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0121
432 D(4) dopamine receptor DRD4 0.0117
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0111
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0108
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0105
3941 Amine oxidase [flavin-containing] A MAOA 0.0104
6145 Solute carrier family 22 member 1 SLC22A1 0.0099
6016 Cytochrome P450 2C19 CYP2C19 0.0093
638 D(3) dopamine receptor DRD3 0.0091
716 5-hydroxytryptamine 7 receptor HTR7 0.0083
163 D(1B) dopamine receptor DRD5 0.0081
725 5-hydroxytryptamine 1D receptor HTR1D 0.008
1256 5-hydroxytryptamine 6 receptor HTR6 0.008
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0078
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0078
6013 Cytochrome P450 2E1 CYP2E1 0.0077
3923 Cholinesterase BCHE 0.0076
6030 Cytochrome P450 2B6 CYP2B6 0.0069
4757 Cytochrome P450 2C9 CYP2C9 0.0067
885 5-hydroxytryptamine 1B receptor HTR1B 0.0066
4118 Cytochrome P450 3A5 CYP3A5 0.0064
587 Serum albumin ALB 0.0059
465 Calmodulin CALM1 0.0058
6144 Solute carrier family 22 member 2 SLC22A2 0.0056
6147 Solute carrier family 22 member 3 SLC22A3 0.0052
6107 Cytochrome P450 3A7 CYP3A7 0.005
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0049
828 Phenylalanine-4-hydroxylase PAH 0.0046
3109 Phenylalanine-4-hydroxylase phhA 0.0046
6138 Multidrug resistance protein 3 ABCB4 0.0043
1636 Trace amine-associated receptor 1 TAAR1 0.0039
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0038
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0038
3426 Glutamine synthetase glnA 0.0037
3987 Glutamine synthetase GLUL 0.0037
124 Histamine H2 receptor HRH2 0.0037
528 5-hydroxytryptamine 1E receptor HTR1E 0.0037
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0036
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0035
6859 Protein S100-A4 S100A4 0.0035
436 5-hydroxytryptamine 2B receptor HTR2B 0.0035
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0034
474 Acetylcholinesterase ACHE 0.0032
1517 Beta-3 adrenergic receptor ADRB3 0.0031
4120 NADPH--cytochrome P450 reductase POR 0.003
341 5-hydroxytryptamine 3 receptor HTR3A 0.0029
3947 Xanthine dehydrogenase/oxidase XDH 0.0028
118 Organic cation/carnitine transporter 2 SLC22A5 0.0025
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0024
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0024
6024 Cytochrome P450 1A1 CYP1A1 0.0022
4924 Cytochrome P450 2C8 CYP2C8 0.0022
3939 Amine oxidase [flavin-containing] B MAOB 0.0021
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
6164 POU domain, class 5, transcription factor 1 POU5F1 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
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0017
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0017
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0017
1656 CYP2B protein CYP2B 0.0017
194 NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2 0.0016
183 Vascular endothelial growth factor A VEGFA 0.0014
20 Prostaglandin G/H synthase 1 PTGS1 0.0014
233 Potassium channel subfamily K member 2 KCNK2 0.0014
6151 Monocarboxylate transporter 10 SLC16A10 0.0012
6106 Cytochrome P450 2C18 CYP2C18 0.0012
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
833 Organic cation/carnitine transporter 1 SLC22A4 0.0012
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0012
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0012
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0012
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0011
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0011
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0011
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0011
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0011
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0011
158 Sodium channel protein type 1 subunit alpha SCN1A 0.001
776 Bile salt export pump ABCB11 0.001
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0009
5718 Cytochrome P450 2A6 CYP2A6 0.0009
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0008
1618 High affinity nerve growth factor receptor NTRK1 0.0008
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0008
164 Histamine H4 receptor HRH4 0.0007
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
1898 Cytochrome P450 1B1 CYP1B1 0.0004
↑