By John R. Fozard (auth.), Pier Andrea Borea (eds.)
This booklet "A3 Adenosine Receptors from phone Biology to Pharmacology and Therapeutics " files the current kingdom of information of the adenosine A3 receptor. Adenosine A3 receptors are G protein-linked receptors that functionality in body structure and intracellular signaling and are considering inflammatory responses and mediating phone proliferation and mobilephone loss of life.
The A3 receptor is more and more being famous for its organic roles in the course of the physique, and plenty of A3 receptor ligands have confirmed priceless in elucidating peripheral and relevant pathologies. This booklet covers a variety of info together with information from reports of theoretical, molecular and mobile pharmacology, sign transduction, integrative body structure, new drug discoveries and scientific purposes. The booklet contains sections on:
- A3 Adenosine Receptor sign transduction
- Adenosine Receptor medicinal chemistry
- Effects and healing purposes 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 technological know-how and suitable purposes and supply an authoritative account of the present prestige of the sector. "A3 Adenosine Receptors from phone Biology to Pharmacology and Therapeutics" is an up to the moment and scientifically very good resource of data, beautiful to easy and scientific scientists alike.
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ISBN: 0781797667 | ISBN-13: 9780781797665 | eISBN: 1451158785 | eISBN-13: 9781451158786 | version: 6
Publication Date: March 2010
Publisher: Lippincott Williams & Wilkins
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Extra info for A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics
J Allergy Clin Immunol 88:951–960 Elwood W, Lötval JO, Barnes PJ, Fan Chung K (1992) Effect of dexamethasone and cyclosporin A on allergen-induced airway hyperresponsiveness and inflammatory cell responses in sensitised Brown Norway rats. Am Rev Resp Dis 145:1289–1294 Elwood W, Barnes PJ, Sakamoto T, Fan Chung K (1993) Allergen-induced airway hyperresponsiveness in Brown Norway rat: role of parasympathetic mechanisms. J Appl Physiol 75:279–284 Ezeamuzie CI, Philips E (2003) Positive coupling of atypical adenosine A3 receptors on human eosinophils to adenylyl cyclase.
As for the glycine receptor, the agonist binding has to be classified as entropy-driven (2 £ DH° £ 20 kJ/mol; −56 £ −TDS° £ −25 kJ/mol), whereas the antagonist binding is mostly enthalpy-driven (−58 £ DH° £ −15 kJ/mol; −15 £ −TDS° £ 29 kJ/mol) (Gomez et al. 1989). Agonist binding to the GABAA receptor is entropy-driven (−1 £ DH° £ 14 kJ/mol; −48 £ −TDS° £ −28 kJ/mol) while antagonist binding is enthalpy- and entropy-driven (−23 £ DH° £ −12 kJ/mol; −31 £ −TDS° £ −15 kJ/mol) (Maksai 1994). A similar result is also obtained for the serotonin 5HT3 receptor where the agonist binding is totally entropy-driven (18 £ DH° £ 53 kJ/mol; −95 £ −TDS° £ −60 kJ/mol) and antagonist binding is both enthalpy- and entropy-driven (−16 £ DH° £ 0 kJ/mol; −53 £ −TDS° £ −21 kJ/mol) (Borea et al.
On this basis, we decided to re-evaluate the effects of CPA and 2-Cl-IB-MECA at concentrations higher than those used previously. 6). 5). 3 mg kg−1; filled columns) or saline (open columns). Responses are expressed relative to the response to bethanechol (100 mM) which was taken as 100%. Mean values (± SEM) from the number of individual experiments shown in parentheses are presented. R. 1 + 1 (6) Cl-IB-MECA Methysergide Cl-IB-MECA DPCPX Cl-IB-MECA + + + Methysergide Methysergide DPCPX Fig. 3 mg kg−1 intratracheally).
A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics by John R. Fozard (auth.), Pier Andrea Borea (eds.)