The 5-HT1D receptor antagonist GR 127,935 is an agonist at cloned human 5-HT1D alpha receptor sites.
The cAMP response of the 5-HT1D receptor antagonist GR 127,935 was compared with 5-CT and ketanserin at cloned human 5-HT1D alpha receptor sites in transfected C6-glial cells. GR 127,935 showed marked agonist activity (EC50-value: 141 nM), its maximal effect being comparable to that of the agonist 5-CT (EC50-value: 0.91 nM), unlike the apparently silent antagonist ketanserin (KB-value: 34 nM).
Pauwels
P J
PJ
Centre de Recherche Pierre Fabre, Laboratory of Cellular and Molecular Neurobiology, Castres, France.
Colpaert
F C
FC
D000818:Animals; D002478:Cells, Cultured / Q000187:drug effects; D003001:Cloning, Molecular; D005576:Colforsin / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006801:Humans; D010069:Oxadiazoles / Q000494:pharmacology*; D010879:Piperazines / Q000494:pharmacology*; D051381:Rats; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000494:pharmacology*
D010069:Oxadiazoles; D010879:Piperazines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D005576:Colforsin; C090701:GR 127935; D000242:Cyclic AMP