Adenosine receptor antagonists

Melatonin [73-31-4] C 2H N202 (31) has marked effects on circadian rhythm (11). Novel ligands for melatonin receptors such as (32) (12), C2yH2gN202, have affinities in the range of 10 Af, and have potential use as therapeutic agents in the treatment of the sleep disorders associated with jet lag. Such agents may also be usehil in the treatment of seasonal affective disorder (SAD), the depression associated with the winter months. Histamine (see Histamine and histamine antagonists), adenosine (see Nucleic acids), and neuropeptides such as corticotropin-like intermediate lobe peptide (CLIP) and vasoactive intestinal polypeptide (VIP) have also been reported to have sedative—hypnotic activities (7). 

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... 

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. 

Derivatives of 2,4-dioxopurine, which may act as adenosine receptor antagonists, depending on the chemical structure. 

Rail, T. W., Evolution of the mechanism of action of methylxanthines From calcium mobilizers to antagonists of adenosine receptors, Pharmacologist, 24, 277, 1982. 

The main mechanism of action of caffeine occurs via the blockade of adenosine receptors in the CNS. Adenosine is an autacoid, which is involved in the modulation of behavior, oxygenation of cells, and dilatation of cerebral and coronary blood vessels and indirectly inhibits the release of dopamine. The blockade of adenosine receptors by caffeine increases the activity of dopamine, which is implicated in the effects of caffeine (91). The question that arises from this observation is to know whether or not adenosine antagonists hold potential for the treatment of Parkinsonism, and further study on the adenosine receptor antagonists from medicinal plants should be encouraged. A possible source for such agents could be the medicinal flora of Asia and the Pacific, among which is the family Sapindaceae. 

Fredholm B. B., Lindstrom K (1999). Autoradiographic comparison of the potency of several structurally unrelated adenosine receptor antagonists at adenosine Al and A(2A) receptors. Eur. J. Pharmacol. 380, 197-202. 

Harper L. K., Beckett S. R., Marsden C. A., McCreary A. C., Alexander S. P. (2006). Effects of the A(2A) adenosine receptor antagonist KW6002 in the nucleus accumbens in vitro and in vivo. Pharmacol Biochem. Behav. in press. 

The synthesis and biological studies of a new series of pyrazolo[4,3-e][l,2,4]triazolo[l,5-cjpyrimidines as antagonists of the human A3 adenosine receptor have been reported <06JMC1720>. 

TABLE 17-2 Subtypes of adenosine receptor, their effectors and selective agonists and antagonists ... 

FIGURE 17-7 The structures of selective agonists and antagonists of adenosine receptors. 

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