58 products were found matching "K04265"!

DPCPX is an adenosine A1 receptor antagonist (Ki = 0.3 nM). It is selective for the adenosine A1 receptor over the adenosine A2 receptor (Ki = 340 nM). DPCPX (0.03 and 1 µM) increases the force of contractions in isolated guinea pig left auricles and inhibits decreases in contraction forces induced by the adenosine...

MIPS521 is an adenosine A1 receptor positive allosteric modulator. It binds to adenosine A1 receptors (Kb = 11 µM) and enhances adenosine-induced inhibition of forskolin-induced cAMP production in CHO cells expressing recombinant human adenosine A1 receptors when used at concentrations ranging from 0.3 to 30 µM. In...

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat ADORA1. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat ADORA1. Next,...

5'-N-Ethylcarboxamidoadenosine (NECA) is an adenosine analog that acts as an agonist of adenosine receptors (Kis = 1,880, 6,660, and 3.5 nM for human adenosine subtypes A1, A2A, and A3, respectively). NECA is reported to act as a potent vasodilator and can inhibit platelet aggregation by increasing cAMP (EC50 = 3.1...

2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively. CADO has been used to activate adenosine receptors in the thalamus, generating anticonvulsive activity in a rat model of generalized...

Theobromine is a methylxanthine alkaloid and derivative of caffeine (Cay-14118) that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist (IC50s = 200-280 µM in radioligand binding assays using rat brain membranes). Theobromine (150 µg/ml) increases AMPK...

Caffeine is a methylxanthine alkaloid naturally found in various plant parts that acts as an antagonist at central adenosine receptors at relevant physiological concentrations (IC50 = ~30 µM). It alters fatigue, mood, alertness, motor reaction time, vascular hemodynamics, and pain sensation. Caffeine has also been...

5'-Deoxy-5'-methylthioadenosine (MTA) is an intermediate in the generation of adenine and methionine that is produced by the decarboxylation of S-adenosylmethionine. This nucleoside is a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 µM for A1, A2A, A2B, and A3, respectively). At higher...

7-Methylxanthine is an adenosine A1 receptor antagonist and active metabolite of theobromine (Cay-21745) and caffeine (Cay-14118). It inhibits binding of the adenosine A1 receptor agonist cyclohexyladenosine in rat cerebral cortical membranes in a concentration-dependent manner. 7-Methylxanthine (300 mg/kg) inhibits...

KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM). It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1, Ki = 7.82 µM). KW 3902 exhibits renal protective effects during...

N6-Cyclopentyladenosine is a selective agonist at adenosine 1 receptors (A1Rs) (Kis = 2.3, 790, and 43 nM for A1R, A2R, and A3R receptors, respectively, in transfected CHO cells). When microinjected into the rat brainstem, it increases blood pressure and heart rate. It is effective for pain in normal and...

5'-Deoxy-5'-methylthioadenosine-d3 (MTA-d3) is intended for use as an internal standard for the quantification of MTA (Cay-15593) by GC- or LC-MS. MTA is an intermediate in the generation of adenine and methionine that is produced by the decarboxylation of S-adenosylmethionine. This nucleoside is a potent agonist of...