Chemical Name:(2-Amino-4,5-dimethyl-3-thienyl)-[3-(trifluoromethyl)ph
enyl]methanone
Biological Activity:
Allosteric
potentiator at the adenosine A1 receptor; acts via agonist-dependent
and -independent mechanisms. Enhances agonist affinity for, and increased t1/2
of dissociation from, the receptor. Also inhibits basal and
forskolin-stimulated adenylyl cyclase (AC) activity in A1 receptors
expressed in CHO cells, possibly via direct potentiation of constitutive
receptor activity or by direct inhibition of AC. Active in vivo.
Brunset al (1990) Structure-activity relationships for
enhancement of adenosine A1 receptor binding by
2-amino-3-benzoylthiophenes. Mol.Pharmacol. 38 950.Mizumuraet al (1996) PD
81,723, an allosteric enhancer of the A1 adenosine receptor, lowers
the threshold for ischemic preconditioning in dogs. Circ.Res. 79
415. Kollias-Bakeret al (1997) Agonist-independent effect of an
allosteric enhancer of the A1 adenosine receptor in CHO cells stably
expressing the recombinant human A1 receptor. J.Pharmacol.Exp.Ther. 281
761. Musseret al (1999) Adenosine A1
receptor-dependent and -independent effects of the allosteric enhancer PD
81,723. J.Pharmacol.Exp.Ther. 288 446.
