THE 5-HT1D RECEPTOR ANTAGONIST GR-127,935 IS AN AGONIST AT CLONED HUMAN 5-HT1D-ALPHA RECEPTOR-SITES

Authors
PAUWELS PJ COLPAERT FC
Citation
Pj. Pauwels et Fc. Colpaert, THE 5-HT1D RECEPTOR ANTAGONIST GR-127,935 IS AN AGONIST AT CLONED HUMAN 5-HT1D-ALPHA RECEPTOR-SITES, Neuropharmacology, 34(2), 1995, pp. 235-237
Citations number
10
Categorie Soggetti
Pharmacology & Pharmacy",Neurosciences
Journal title
Neuropharmacology → ACNP
ISSN journal
00283908
Volume
34
Issue
2
Year of publication
1995
Pages
235 - 237
Database
ISI
SICI code
0028-3908(1995)34:2<235:T5RAGI>2.0.ZU;2-I
Abstract
The cAMP response of the 5-HT1D receptor antagonist GR 127,935 was com pared with 5-CT and ketanserin at cloned human 5-HT1D alpha receptor s ites in transfected C6-glial cells. GR 127,935 showed marked agonist a ctivity (EC(50)-value: 141 nM), its maximal effect being comparable to that of the agonist 5-CT (EC(50)-value: 0.91 nM), unlike the apparent ly silent antagonist ketanserin (K-B-value: 34 nM).