Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.
Acylated and aroylated hydrazinoclozapines are highly potent dopamine D(1) antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D(1)K(i) of 1.6 nM and 212-fold selectivity over D(2) receptor.
Sasikumar
T K
TK
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com
Burnett
D A
DA
Zhang
H
H
Smith-Torhan
A
A
Fawzi
A
A
Lachowicz
J E
JE
D003024:Clozapine / Q000138:chemical synthesis / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000145:classification / Q000494:pharmacology*; D065127:Dopamine D2 Receptor Antagonists; D006834:Hydrazines / Q000737:chemistry*; D015394:Molecular Structure; D017447:Receptors, Dopamine D1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D013329:Structure-Activity Relationship
D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D006834:Hydrazines; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; C029424:hydrazine; D003024:Clozapine