Substituent effects of N-(1, 3-diphenyl-1 H-pyrazol-5-yl) benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes

…, K Hemstapat, Y Chen, Y Zhang, S Saleh…

Index: De Paulis, Tomas; Hemstapat, Kamondanai; Chen, Yelin; Zhang, Yongqin; Saleh, Samir; Alagille, David; Baldwin, Ronald M.; Tamagnan, Gilles D.; Conn, P. Jeffrey Journal of Medicinal Chemistry, 2006 , vol. 49, # 11 p. 3332 - 3344

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Citation Number: 96

Abstract

CDPPB [3-cyano-N-(1, 3-diphenyl-1 H-pyrazol-5-yl) benzamide] was recently described as the first centrally active, positive allosteric modulator of rat and human metabotropic glutamate receptor (mGluR) mGluR5 subtype. We explored the structural requirements for potentiation of glutamate-induced calcium release in naturally expressed mGluR5 in cultured rat astrocytes and increasing affinity for the allosteric antagonist binding site by ...