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Overview
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Background
BRL-15572 is an antagonist of 5-HT1D receptor with pKi value of 7.9 [1].In the in vitro binding assay, BRL-15572 shows 60-fold higher affinity for human 5-HT1D receptor than for h5-HT1B receptor. However, it also has moderately high affinity at both human 5-HT1A and human 5-HT2B receptors. It limits the use of BRL-15572 as a pharmacological tool in systems. In native tissue, BRL-15572 totally inhibits [3H] 5-CT specific binding in guinea-pig striatum. In the functional assays, BRL-15572 is potent at both [35S] GTPγS binding assay and cAMP accumulation assay. It shows a pEC50 value of 8.1 at h5-HT1D receptor expressed in CHO cell membranes. And the activity shows to be lower in the cAMP assay [1].
[1] Price G W, Burton M J, Collin L J, et al. SB-216641 and BRL-15572–compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn-Schmiedeberg's archives of pharmacology, 1997, 356(3): 312-320.
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