Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1 alpha metabotropic glutamate receptor

Hermans, Emmanuel;Nahorski, SR;Challiss, RAJ
(1998) Neuropharmacology — Vol. 37, n° 12, p. 1645-1647 (1998)

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In transfected CHO cells expressing the human metabotropic glutamate receptor mGlu1 alpha, 7- hydroxyimino)cyclopropan[b]chromen-1a-carboxylic acid ethylester (CPCCOEt) was found to antagonize L-quisqualate-induced phosphoinositide hydrolysis in a non-competitive and reversible manner (apparent pK(i) value, 4.76 +/- 0.18: It = 3. This suggests that CPCCOEt antagonizes type Ir metabotropic glutamate receptor activation by interacting with a site distinct from the agonist binding site. (C) 1998 Elsevier Science Ltd. All rights reserved.
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Hermans, E., Nahorski, S., & Challiss, R. (1998). Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1 alpha metabotropic glutamate receptor. Neuropharmacology, 37(12), 1645-1647. https://doi.org/10.1016/S0028-3908(98)00132-4 (Original work published 1998)