Cat. No. 1363
Chemical Name: (2-Amino-4,5-dimethyl-3-thienyl)-[3
Biological ActivityAllosteric potentiator at the adenosine A1 receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t½ 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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Musser et al (1999) Adenosine A1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723. J.Pharmacol.Exp.Ther. 288 446. PMID: 9918544.
Kollias-Baker et 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. PMID: 9152383.
Mizumura et 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. PMID: 8781475.
Bruns et al (1990) Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes. Mol.Pharmacol. 38 950. PMID: 2250667.
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Keywords: PD 81723, supplier, Allosteric, potentiators, A1, receptors, Receptors, adenosines, PD81723, Tocris Bioscience, Adenosine A1 Receptor Modulator products
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