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Functional characterisation of a 5HT 2 receptor cDNA cloned from Lymnaea stagnalis

Functional characterisation of a 5HT 2 receptor cDNA cloned from Lymnaea stagnalis,10.1016/0014-2999(96)00410-4,European Journal of Pharmacology,Cindy

Functional characterisation of a 5HT 2 receptor cDNA cloned from Lymnaea stagnalis   (Citations: 15)
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A G-protein-coupled receptor (5-HT2Lym) resembling members of the 5-HT2 receptor subfamily was cloned from the mollusc Lymnaea stagnalis. Serotonin induces a concentration-dependent increase in intracellular inositol phospates in HEK293 cells expressing this receptor (EC50 = 114 nM). 5-HT2Lym differs from mammalian 5-HT2 receptors by the presence of a large amino-terminal region. This large domain appears to preclude an adequate level of expression of 5-HT2Lym in HEK293. Therefore, we constructed a cDNA encoding an amino-terminally truncated receptor (ΔN-5-HT2Lym) that appeared to be much better expressed in HEK293 cells. ΔN-5HT2Lym-expressing cells exhibit a serotonin-induced stimulation of phosphatidylinositol bisphosphate hydrolysis (EC50 = 11.4 nM) and a high-affinity binding of the 5-HT2-selective antagonist [3H]mesulergine (Kd = 4 nM). Inhibition of this binding by several 5-HT2 antagonists and agonists revealed a pharmacological profile most closely resembling those of 5HT2Dro, 5-HT2B and 5-HT2C.
Journal: European Journal of Pharmacology - EUR J PHARMACOL , vol. 311, no. 2, pp. 249-258, 1996
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