Adenosine receptor agonists antagonists

Abscissae, 254f Absolute stoichiometry, 180 Adenosine receptor agonists, 70 Adenylate cyclase, 23, 25f 62-Adrenoceptor antagonists, 4 6-Adrenoceptors, 82 Adsorption process... 

Adenosine Receptors. Table 2 Affinity of commonly used adenosine receptor agonists and antagonists for defining pharmacologically adenosine receptor subtypes... 

Fig. 2.1 van t Hoff plots showing the effect of temperature on the equilibrium binding association constants, KA, for [3H]-MRE 3008F20 in various cell lines examined (a) and for six adenosine receptor agonists (b) and antagonists (c) studied. All plots are essentially linear (r in the range 0.91-0.99) in the temperature range of 0-30°C... 

Cosyn L, Palaniappan KK, Kim SK, Duong HT, Gao ZG, Jacobson KA, Van Calenbergh S (2006b) 2-Triazole-substituted adenosines a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem 49(25) 7373-7383... 

Triazole-substituted adenosines a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem 49 7373-7383... 

Fig. 13.1 Cytoprotective action of adenosine in a quantitative model of mouse hindlimb ischemia and reperfusion (I/R) injury. Adult wild type mice were injected with (a) sterile vehicle (0.1% DMSO in phosphate-buffered saline, pH 7.4) or various adenosine receptor agonists (b, c) or antagonist (d, f). (a) Following ischemia and reperfusion, skeletal muscle showed a significant uptake of Evans Blue dye (EBD) in vehicle-treated mice (first part of (a), representative of 7 mice). The contra-lateral leg not subjected to ischemia-reperfusion showed virtually no EBD uptake. In the second part of (a), the same section was stained with rabbit polyclonal anti-skeletal muscle actin antibodies followed by staining with goat anti-rabbit IgG conjugated with FITC. (b) The nonselective adenosine agonist R-PIA caused a large reduction in the EBD-stained area (see both first and second parts to this figure, representative of six mice)...

Ma, H., Green, R.D., 1992. Modulation of cardiac cyclic AMP metabolism by adenosine receptor agonists and antagonists. Mol. Pharmacol. 42, 831-837. 

Our observations suggest that [ H]chloroadenosine, an adenosine receptor agonist, identifies binding sites in human placenta with characteristics of the high affinity, adenosine receptor. The binding is time dependent, reversible and saturable. The potency series of adenosine receptor methylxanthine antagonists in displacing C Hi chloroadenosine is appropriate. 

PI (adenosine) receptors were explored as therapeutic targets before P2 receptors. Adenosine was identified early and is in current use to treat supraventricular tachycardia. A2a receptor antagonists are being investigated for the treatment of Parkinson s disease and patents have been lodged for the application of PI receptor subtype agonists and antagonists for myocardial ischaemia and reperfusion injury, cerebral ischaemia, stroke, intermittent claudication and renal insufficiency. 

Pharmacological experiments have shown that adenosine and its receptor agonists promote, whereas its antagonists inhibit, sleep. Early experiments showed that injection into the cerebral ventricles of 2 pmol (0.5 mg) adenosine... 

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