By John R. Fozard (auth.), Pier Andrea Borea (eds.)
This booklet "A3 Adenosine Receptors from phone Biology to Pharmacology and Therapeutics " records the current nation of data of the adenosine A3 receptor. Adenosine A3 receptors are G protein-linked receptors that functionality in body structure and intracellular signaling and are eager about inflammatory responses and mediating telephone proliferation and cellphone dying.
The A3 receptor is more and more being famous for its organic roles through the physique, and plenty of A3 receptor ligands have confirmed important in elucidating peripheral and principal pathologies. This e-book covers a variety of info together with facts from experiences of theoretical, molecular and mobile pharmacology, sign transduction, integrative body structure, new drug discoveries and medical functions. The e-book contains sections on:
- A3 Adenosine Receptor sign transduction
- Adenosine Receptor medicinal chemistry
- Effects and healing functions of Adenosine Receptors on tissues and organs
- Adenosine Receptors and inflammatory and auto-immune diseases
- Adenosine Receptors and cancer
The chapters during this publication hide either basic technology and suitable purposes and supply an authoritative account of the present prestige of the sector. "A3 Adenosine Receptors from cellphone Biology to Pharmacology and Therapeutics" is an up to the moment and scientifically first-class resource of knowledge, beautiful to uncomplicated and medical scientists alike.
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Extra info for A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics
15 Thermodynamic parameters DG°, DH° and DS° are expressed as means ± SEM, temperature used was 25°C. 11 Thermodynamic parameters DG°, DH° and DS° are expressed as means ± SEM, temperature used was 25°C. and from −52 to −9 kJ/mol and DS° values from 225 to 410 J/K/mol and from 16 to 81 J/K/mol for agonists and antagonists, respectively. 15 K). It becomes apparent that all points are arranged on the same diagonal band encompassed between the two dashed lines which represent the loci of points defined by the limiting KD values of 100 µM and 10 pM.
J Appl Physiol 75:279–284 Ezeamuzie CI, Philips E (2003) Positive coupling of atypical adenosine A3 receptors on human eosinophils to adenylyl cyclase. Biochem Biophys Res Commun 300:712–718 Feoktistov I, Biaggioni I (1995) Adenosine A2b receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. J Clin Invest 96:1979–1986 Feoktistov I, Biaggioni I (1997a) Role of adenosine in asthma. Drug Dev Res 39:333–336 Feoktistov I, Biaggioni I (1997b) Adenosine A2B receptors.
As for the membrane receptors it has been demonstrated that A1, A2A, A2B and A3 adenosine receptors are thermodynamically discriminated and agonist binding is entropy-driven and antagonists have enthalpy–entropy driven binding (Borea et al. 1994, 1996a, 2001; Gessi et al. 2008b; Merighi et al. 2002; Varani et al. 2000, 2008a). In addition, five out of six ligand-gated ion channel receptors (LGICR), that is glycine, GABA, serotonin 5HT3, neuronal nicotinic and purinergic P2X3 receptors discriminate in vitro agonists from antagonists (Gomez et al.