Abstract
A clone, G-21, was isolated from a human genomic library by cross-hybridization with the β2-adrenergic receptor cDNA [Kobilka et al. (1987) Nature 329, 75–79]. The encoded protein, transiently expressed in monkey kidney cells (COS-7 cells) displays the binding characteristics of the 5-HT1A receptor (5-HT1AR). Using a combination of photoaffinity labeling with the ligand [125I]-N3-NAPS and immunoprecipitation with an antipeptide antiserum (JWR21), we have determined by SDS-PAGE that the molecular weights of the 5-HT1AR from both transfected COS-7 cells and human hippocampus, are respectively 75 and 64 kDa. The 5-HT1AR was also transfected into HeLa cells and a stably expressing clonal cell line, HA7 (0.5 pmol receptor/mg protein), was utilized to characterize the second messenger coupling of the 5-HT1AR. 5-HT did not stimulate adenylyl cyclase (AC) but rather inhibited forskolin-induced cAMP formation (EC50≈20 nM). Surprisingly, in these cells 5-HT also activated phosphatidylinositol hydrolysis, but with less potency (EC50≈3.2 µM).
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Fargin, A., Raymond, J.R., Lefkowitz, R.J., Caron, M.G. (1990). Biochemical Characterization of the Cloned Human 5-HT1A Receptor Expressed in Mammalian Cells. In: Paoletti, R., Vanhoutte, P.M., Brunello, N., Maggi, F.M. (eds) Serotonin. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-1912-9_4
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DOI: https://doi.org/10.1007/978-94-009-1912-9_4
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