Inhibition of rabbit monoamine oxidase by doxepin and related drugs

Jerome A. Roth

doi:10.1016/0024-3205(75)90316-1

Inhibition of rabbit monoamine oxidase by doxepin and related drugs

Jerome A. Roth

Pharmacology and Toxicology

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13 Scopus citations

Abstract

The psychotherapeutic agent, doxepin, inhibits both the B and A forms of rabbit lung mitochondrial monoamine oxidase (MAO). The K_i values for doxepin inhibition of phenylethylamine (PEA) and 5-hydroxytryptamine (5-HT) deamination is 3 × 10^-5 and 2 × 10^-4M, respectively. Doxepin is, thus, similar to other tricyclic antidepressant drugs in that it has a greater affinity for the B form of the rabbit oxidase. The ability of doxepin and imipramine and its mono and didesmethyl derivatives to inhibit rabbit MAO is decreased as the pH is raised above 8.0. However, results suggest that the basicity of the propylamine side chain has little or no influence on the ability of these drugs to inhibit the rabbit oxidase. In addition, it is demonstrated that 7 × 10^-6M doxepin inhibits PEA deamination by human platelet MAO approximately 50%.

Original language	English
Pages (from-to)	1309-1319
Number of pages	11
Journal	Life Sciences
Volume	16
Issue number	8
DOIs	https://doi.org/10.1016/0024-3205(75)90316-1
State	Published - Apr 15 1975

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title = "Inhibition of rabbit monoamine oxidase by doxepin and related drugs",

abstract = "The psychotherapeutic agent, doxepin, inhibits both the B and A forms of rabbit lung mitochondrial monoamine oxidase (MAO). The Ki values for doxepin inhibition of phenylethylamine (PEA) and 5-hydroxytryptamine (5-HT) deamination is 3 {\texttimes} 10-5 and 2 {\texttimes} 10-4M, respectively. Doxepin is, thus, similar to other tricyclic antidepressant drugs in that it has a greater affinity for the B form of the rabbit oxidase. The ability of doxepin and imipramine and its mono and didesmethyl derivatives to inhibit rabbit MAO is decreased as the pH is raised above 8.0. However, results suggest that the basicity of the propylamine side chain has little or no influence on the ability of these drugs to inhibit the rabbit oxidase. In addition, it is demonstrated that 7 {\texttimes} 10-6M doxepin inhibits PEA deamination by human platelet MAO approximately 50\%.",

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T1 - Inhibition of rabbit monoamine oxidase by doxepin and related drugs

AU - Roth, Jerome A.

PY - 1975/4/15

Y1 - 1975/4/15

N2 - The psychotherapeutic agent, doxepin, inhibits both the B and A forms of rabbit lung mitochondrial monoamine oxidase (MAO). The Ki values for doxepin inhibition of phenylethylamine (PEA) and 5-hydroxytryptamine (5-HT) deamination is 3 × 10-5 and 2 × 10-4M, respectively. Doxepin is, thus, similar to other tricyclic antidepressant drugs in that it has a greater affinity for the B form of the rabbit oxidase. The ability of doxepin and imipramine and its mono and didesmethyl derivatives to inhibit rabbit MAO is decreased as the pH is raised above 8.0. However, results suggest that the basicity of the propylamine side chain has little or no influence on the ability of these drugs to inhibit the rabbit oxidase. In addition, it is demonstrated that 7 × 10-6M doxepin inhibits PEA deamination by human platelet MAO approximately 50%.

AB - The psychotherapeutic agent, doxepin, inhibits both the B and A forms of rabbit lung mitochondrial monoamine oxidase (MAO). The Ki values for doxepin inhibition of phenylethylamine (PEA) and 5-hydroxytryptamine (5-HT) deamination is 3 × 10-5 and 2 × 10-4M, respectively. Doxepin is, thus, similar to other tricyclic antidepressant drugs in that it has a greater affinity for the B form of the rabbit oxidase. The ability of doxepin and imipramine and its mono and didesmethyl derivatives to inhibit rabbit MAO is decreased as the pH is raised above 8.0. However, results suggest that the basicity of the propylamine side chain has little or no influence on the ability of these drugs to inhibit the rabbit oxidase. In addition, it is demonstrated that 7 × 10-6M doxepin inhibits PEA deamination by human platelet MAO approximately 50%.

UR - https://www.scopus.com/pages/publications/0016852601

U2 - 10.1016/0024-3205(75)90316-1

DO - 10.1016/0024-3205(75)90316-1

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VL - 16

SP - 1309

EP - 1319

JO - Life Sciences

JF - Life Sciences

IS - 8

ER -

Inhibition of rabbit monoamine oxidase by doxepin and related drugs

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