Article
Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor.
Biochemical pharmacology - 15 Jan 2001
Kourounakis A, Visser C, de Groote M, IJzerman A P
Abstract excerpt
The 2-amino-benzoylthiophene derivative PD81,723 [(2-amino-4,5-dimethyl-trienyl)[3-(trifluoromethyl) phenyl]methanone] has been shown to allosterically enhance agonist binding and function at the adenosine A(1) receptor. The aim of the present study was to elucidate the effects of PD81,723 both as an allosteric enhancer and as an antagonist on the adenosine A(1) receptor. We investigated its effect on the human...
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