Cloned human 5-HT1A receptor pharmacology determined using agonist binding and measurement of cAMP accumulation

Twenty agonists and nine antagonists were evaluated for their ability to compete for [3H]‐8‐hydroxy‐2‐(di‐n‐propylamino)tetralin ([3H]‐8‐OH‐DPAT) binding to the cloned human serotonin‐1A (ch‐5‐HT1A) receptor expressed in Chinese hamster ovary cells and for their ability to alter adenylyl cyclase activity in the same cells. The most potent full agonists of high affinity included N,N‐dipropyl‐5‐carboxamidotryptamine (pEC50 = 9.6 ± 0.1), MDL 73005EF (pEC50 = 9.3 ± 0.2), 5‐methyl‐urapidil (pEC50 = 9.2 ± 0.1), 5‐carboxamidotryptamine (pEC50 = 9.1 ± 0.2), R(+)‐8‐OH‐DPAT (pEC50 = 8.6 ± 0.1) and BMY‐7378 (pEC50 = 8.6 ± 0.1). WB‐4101 (pEC50 = 8.3 ± 0.2; IA = 79%), clozapine (pEC50 = 8.1 ± 0.3; IA = 29%), (buspirone (pEC50 = 7.6 ± 0.2; IA = 79%), quipazine (pEC50