Changes in pharmacology and function of the naturally occurring Phe124Cys variant of the human (h) 5-HT_(1B) receptor in transfected cells and human temporal arteries (HTA)

【Author】

Raphaela Verheggen;Inga Werner;Anne Lücker;Michael Brüss;Alberto Kaumann;Manfred Gthert;

【Abstract】

<正>In competition binding experiments with [3H]5-carboxamidotryptamine ([3H]5-CT) on rat C6 glioma cells expressing either the h5-HT1B Cys-124 variant receptor (VR) or the h5-HT1B wild-type receptor (WR), 5-CT, 5-hydroxytryptamine (5-HT) and sumatriptan exhibited higher affinity for the VR. The potency of 5-CT, 5-HT and sumatriptan in stimulating [35S]GTPgammaS binding to membranes of cells expressing the VR was 2.3 to 3.8-fold higher. In whole C6 cells

【Keywords】

5-HT, 5-HT1B,Cys124Phe mutant, human temporal artery

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