A novel inhibitor of gamma-aminobutyrate aminotransferase with anorectic activity.
1-(n-decyl)-3-Pyrazolidinone (BW357U) is a potent, selective inhibitor of gamma-aminobutyrate aminotransferase (GABA-T) in vitro and in vivo. After acute or chronic, oral or intraperitoneal administration of BW357U to rats, brain GABA levels were elevated in a dose-dependent manner. When inhibition of brain GABA-T exceeded 50%, whole brain GABA levels were elevated approximately threefold, and an anorectic effect was observed in the absence of other symptoms. This compound, because of its potency and selectivity, may be useful in studies relating to the function of GABA-containing neurons in appetite regulation.
D000612:4-Aminobutyrate Transaminase / Q000037:antagonists & inhibitors*; D000818:Animals; D001066:Appetite / Q000187:drug effects*; D001067:Appetite Depressants / Q000494:pharmacology; D001921:Brain / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D011720:Pyrazoles / Q000494:pharmacology*; D051381:Rats; D000637:Transaminases / Q000037:antagonists & inhibitors*; D005680:gamma-Aminobutyric Acid / Q000378:metabolism; D047069:Pyrazolones
D000612:4-Aminobutyrate Transaminase; D001067:Appetite Depressants; D011720:Pyrazoles; D000637:Transaminases; D005680:gamma-Aminobutyric Acid; C034865:1-(n-decyl)-3-pyrazolidinone; D047069:Pyrazolones