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• W1969323982 abstract "Previous studies by another group have suggested that the α2-adrenergic receptor antagonist rauwolscine may function as an agonist at the serotonini1A (5-HT1A) receptor expressed in human brain. To directly test that hypothesis, we transfected the human 5-HT1A receptor cDNA into CHO cells and examined the ability of rauwolscine and its isomer, yohimbine, to inhibit ligand binding of [3H]-(±)-8- hydroxy-2-(di-n-propylamino)tetralin ([3H]8-OH-DPAT) and the activity of adenylyl cyclase in membranes derived from a single transformant that stably expresses ≈225 fmol of 5-HT1A receptor/mg of membrane protein. Both ligands competitively antagonized the binding of [3H]8-OH-DPAT (Ki = 158 ± 69 nM for rauwolscine and 690 ± 223 nM for yohimbine), yielding shallow displacement curves consistent with agonist activity (Hill values = 0.69 ± 0.2 for rauwolscine and 0.63 ± 0.06 for yohimbine). Both ligands also inhibited forskolin-stimulated adenylyl cyclase activity in membranes derived from transfected (but not nontransfected) cells. For rauwolscine, the IC50 was 1.5 ± 0.2 μM, and for yohimbine 4.6 ± 1.0 μM, with activity ratios of 0.70 and 0.59, respectively, when compared to the full agonist serotonin. These studies demonstrated that rauwolscine and yohimbine are partial agonists for the human 5-HT1A receptor." @default.
• W1969323982 created "2016-06-24" @default.
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• W1969323982 date "1993-06-01" @default.
• W1969323982 modified "2023-10-07" @default.
• W1969323982 title "Partial agonist properties of rauwolscine and yohimbine for the inhibition of adenylyl cyclase by recombinant human 5-HT1A receptors" @default.
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• W1969323982 doi "https://doi.org/10.1016/0006-2952(93)90208-e" @default.
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