PHOTOACTIVATABLE ANALOGS OF A SUBSTANCE-P NONPEPTIDIC ANTAGONIST, FORPROBING THE ANTAGONIST BINDING-SITE OF THE NK1 RECEPTOR

Authors
KERSEY ID FISHWICK CWG FINDLAY JBC WARD P
Citation
Id. Kersey et al., PHOTOACTIVATABLE ANALOGS OF A SUBSTANCE-P NONPEPTIDIC ANTAGONIST, FORPROBING THE ANTAGONIST BINDING-SITE OF THE NK1 RECEPTOR, Bioorganic & medicinal chemistry letters, 5(12), 1995, pp. 1271-1274
Citations number
24
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
12
Year of publication
1995
Pages
1271 - 1274
Database
ISI
SICI code
0960-894X(1995)5:12<1271:PAOASN>2.0.ZU;2-I
Abstract
2S,3S)-3-(2-methoxybenzylamino)-2-phenylpiperidine (CP-99,994) binds w ith high affinity (pK(i) 9.6) to the human NK1 receptor. Racemic analo gues of CP-99,994 containing either benzoyl or diazirinyl moieties als o bind with high affinity (pK(i) 9.4 and 9.1 respectively), These anal ogues are of tremendous potential for mapping the antagonist binding s ite of the NK1 receptor.