title: Hydrazides of clozapine: a new class of D1 dopamine receptor subtype selective antagonists.
abstract: 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.
authors.affiliation: Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com
authors.forename: T K
authors.initials: TK
authors.lastname: Sasikumar
authors.forename: D A
authors.initials: DA
authors.lastname: Burnett
authors.forename: H
authors.initials: H
authors.lastname: Zhang
authors.forename: A
authors.initials: A
authors.lastname: Smith-Torhan
authors.forename: A
authors.initials: A
authors.lastname: Fawzi
authors.forename: J E
authors.initials: JE
authors.lastname: Lachowicz
mesh_terms: 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
chemical_list: D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D006834:Hydrazines; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; C029424:hydrazine; D003024:Clozapine