PD 81,723
PD 81,723 structure
|
Common Name | PD 81,723 | ||
|---|---|---|---|---|
| CAS Number | 132861-87-1 | Molecular Weight | 299.31100 | |
| Density | 1.328g/cm3 | Boiling Point | 411.7ºC at 760 mmHg | |
| Molecular Formula | C14H12F3NOS | Melting Point | N/A | |
| MSDS | USA | Flash Point | 202.8ºC | |
|
Endogenous adenosine reduces the occurrence of ischemia-induced ventricular fibrillation in rat heart.
J. Mol. Cell. Cardiol. 31(1) , 123-34, (1999) The aim of this study was to determine whether endogenous adenosine has antiarrhythmic effects on ischemia-induced ventricular tachyarrhythmias. We therefore modulated the effect of endogenous adenosine in isolated rat hearts using four different approaches. ... |
|
|
A1 adenosine receptor allosteric enhancer PD-81723 protects against renal ischemia-reperfusion injury.
Am. J. Physiol. Renal Physiol. 303(5) , F721-32, (2012) Activation of A(1) adenosine receptors (ARs) protects against renal ischemia-reperfusion (I/R) injury by reducing necrosis, apoptosis, and inflammation. However, extrarenal side effects (bradycardia, hypotension, and sedation) may limit A(1)AR agonist therapy... |
|
|
Novel mitogenic effect of adenosine on coronary artery smooth muscle cells: role for the A1 adenosine receptor.
Circ. Res. 96(9) , 982-90, (2005) Adenosine is a vascular endothelial cell mitogen, but anti-mitogenic for aortic smooth muscle cells and fibroblasts when acting via the A2B adenosine receptor. However, we show that adenosine increases porcine coronary artery smooth muscle cell (CASMC) number... |
|
|
Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor.
Bioorg. Med. Chem. Lett. 10(17) , 1953-7, (2000) New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81,723 and at a concentration of 0.1 ... |
|
|
Enhancer and competitive allosteric modulation model for G-protein-coupled receptors
J. Theor. Biol. 267(4) , 663-75, (2010) A new mathematical model, referred to as Enhancer and Competitive Allosteric Modulator (ECAM) model, developed with the aim of quantitatively describing the interaction of an allosteric modulator with both enhancer and competitive properties towards G-protein... |
|
|
Inhibition of muscarinic K+ current in guinea-pig atrial myocytes by PD 81,723, an allosteric enhancer of adenosine binding to A1 receptors.
Br. J. Pharmacol. 121(6) , 1217-23, (1997) 1. PD 81,723 has been shown to enhance binding of adenosine to A1 receptors by stabilizing G protein-receptor coupling ('allosteric enhancement'). Evidence has been provided that in the perfused hearts and isolated atria PD 81,723 causes a sensitization to ad... |
|
|
Potentiation of the negative dromotropic effect of adenosine by rapid heart rates: possible ionic mechanism.
Basic Res. Cardiol. 97(4) , 295-304, (2002) Adenosine-induced slowing of atrioventricular nodal conduction is a rate-dependent process that is potentiated by the A(1)-adenosine receptor allosteric enhancer, PD 81,723. The ionic mechanisms underlying these phenomena were investigated in guinea pig isola... |
|
|
The allosteric enhancer PD81,723 increases chimaeric A1/A2A adenosine receptor coupling with Gs.
Biochem. J. 396(1) , 139-46, (2006) PD81,723 {(2-amino-4,5-dimethyl-3-thienyl)-[3-(trifluromethyl)-phenyl]methanone} is a selective allosteric enhancer of the G(i)-coupled A1 AR (adenosine receptor) that is without effect on G(s)-coupled A2A ARs. PD81,723 elicits a decrease in the dissociation ... |
|
|
Microwave-assisted synthesis of thieno[2,3-c]pyridine derivatives as a new series of allosteric enhancers at the adenosine A(1) receptor.
Bioorg. Med. Chem. Lett. 16(21) , 5530-3, (2006) The microwave-assisted aromatization method has been used for the synthesis of a series of novel thieno[2,3-c]pyridines. This rapid method produces compounds in good yield within minutes in comparison with conventional heating method. The synthesized molecule... |
|
|
Regioselective oxidation of 2-amino-3-aroyl-4,5-dialkylthiophenes by DMSO.
Bioorg. Med. Chem. Lett. 14(4) , 929-33, (2004) Solutions of 2-amino-3-aroyl-4,5-dialkylthiophenes in DMSO (dimethyl sulfoxide) undergo regioselective oxidation of benzylic carbon under mild conditions. We describe three examples and propose a mechanism for oxidation. |