Abstract:
:We investigated some in vitro pharmacological properties of a novel human dopamine D2-like receptor antagonist, YM-50001 [(R)-5-chloro-4-cyclopropylacarbonylamino-2-methoxy-N-[1-(3-methox ybenzyl)- 3-pyrrolidinyl]benzamide monooxalate]. Receptor binding studies revealed that YM-50001 had a potent affinity for human D4 receptors (Ki = 5.62 nM). YM-50001 displayed weak or negligible affinity for other neurotransmitter receptors including human D2 and D3 receptors. YM-50001 shifted the dopamine response curve on each human D2-like receptor subtype-mediated low-Km GTPase activity to the right. YM-50001 also exhibited good D4 selectivity with respect to D2-like receptor antagonism in the functional assay. These results indicate that YM-50001 is a novel, potent and selective D4 receptor antagonist.
journal_name
Neuroreportjournal_title
Neuroreportauthors
Hidaka K,Tada S,Matsumoto M,Ohmori J,Maeno K,Yamaguchi Tsubject
Has Abstractpub_date
1996-11-04 00:00:00pages
2543-6issue
15-17eissn
0959-4965issn
1473-558Xjournal_volume
7pub_type
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