Synonyms: GW-791343
Compound class:
Synthetic organic
Comment: GW791343 is an negative allosteric modulator of the human P2X7 receptor, but is a positive modulator of the rat orthologue [1]. Mutational studies suggest that amino acid 95 is a key residue in determining the species difference in antagonist effects [2]. The position 95 residue is phenylalanine in human P2X7 receptors, and leucine in rat.
|
|
References |
1. Michel AD, Chambers LJ, Walter DS. (2008)
Negative and positive allosteric modulators of the P2X(7) receptor. Br J Pharmacol, 153 (4): 737-50. [PMID:18071294] |
2. Michel AD, Clay WC, Ng SW, Roman S, Thompson K, Condreay JP, Hall M, Holbrook J, Livermore D, Senger S. (2008)
Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects. Br J Pharmacol, 155 (5): 738-51. [PMID:18660826] |