Monoamine oxidase-A selective inhibition in human hypothalamus and liver in-vitro by amiflamine and its metabolites

K F Tipton; A M O'Carroll; J M McCrodden; C J Fowler

Monoamine oxidase-A selective inhibition in human hypothalamus and liver in-vitro by amiflamine and its metabolites

K F Tipton, A M O'Carroll, J M McCrodden, C J Fowler

Research output: Contribution to journal › Article (Academic Journal) › peer-review

2 Citations (Scopus)

Abstract

Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 microM (liver) and 0.8, 0.2 and 14 microM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds.

Original language	English
Pages (from-to)	352-4
Number of pages	3
Journal	Journal of Pharmacy and Pharmacology
Volume	37
Issue number	5
Publication status	Published - May 1985

Keywords

Animals
Humans
Hypothalamus
In Vitro Techniques
Kinetics
Liver
Monoamine Oxidase Inhibitors
Phenethylamines
Rats

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@article{5338a5bea9444e3e8456cfaec5195775,

title = "Monoamine oxidase-A selective inhibition in human hypothalamus and liver in-vitro by amiflamine and its metabolites",

abstract = "Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 microM (liver) and 0.8, 0.2 and 14 microM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds.",

keywords = "Animals, Humans, Hypothalamus, In Vitro Techniques, Kinetics, Liver, Monoamine Oxidase Inhibitors, Phenethylamines, Rats",

author = "Tipton, {K F} and O'Carroll, {A M} and McCrodden, {J M} and Fowler, {C J}",

year = "1985",

month = may,

language = "English",

volume = "37",

pages = "352--4",

journal = "Journal of Pharmacy and Pharmacology",

issn = "0022-3573",

publisher = "Wiley",

number = "5",

}

TY - JOUR

T1 - Monoamine oxidase-A selective inhibition in human hypothalamus and liver in-vitro by amiflamine and its metabolites

AU - Tipton, K F

AU - O'Carroll, A M

AU - McCrodden, J M

AU - Fowler, C J

PY - 1985/5

Y1 - 1985/5

N2 - Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 microM (liver) and 0.8, 0.2 and 14 microM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds.

AB - Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 microM (liver) and 0.8, 0.2 and 14 microM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds.

KW - Animals

KW - Humans

KW - Hypothalamus

KW - In Vitro Techniques

KW - Kinetics

KW - Liver

KW - Monoamine Oxidase Inhibitors

KW - Phenethylamines

KW - Rats

M3 - Article (Academic Journal)

C2 - 2862247

VL - 37

SP - 352

EP - 354

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

IS - 5

ER -