Adrenergic receptor structure

Audet M, Bouvier M Insights into signaling from the beta2-adrenergic receptor structure. Nat Chem Biol 2008 4 397. 

Lefkowitz RJ, Stadel JM, Caron MG. Adenylate cyclase-coupled p-adrenergic receptors structure and mechanisms of activation and desensitization. Annu Rev Biochem 1983 52 159-186. 

Comparison of the rhodopsin and beta2 adrenergic receptor structures as templates for GPCR modeling... 

Hanson MA, Cherezov V, Griffith MT, et al. A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure. 2008 16(6) 897-905. 

Risperidone (11) was also included among a a 1-adrenergic receptor antagonists to study a quantitative structure-activity relationship (99BMC2437). A pharmacophore model for atypical antipsychotics, including 11, was established (00MI41). An increased plasma level of 11 and 9-hydroxyrisperidone (12) was observed in combination with paroxetine (01 MI 13). The effect of vanlafaxine on the pharmacokinetics of 11 was reported (99MI13). 

Cotecchia S et al (2004) Structural determinants involved in the activation and regulation of G protein-coupled receptors lessons from the ai -adrenergic receptor sub-types. Biol Cell 96 327-333... 

Piascik MT, Perez DM (2007) Structure-function of ai-adrenergic receptors. Biochem Phannacol 73 1051-1062... 

ORGANS OR STRUCTURES SYMPATHETIC (ADRENERGIC) EFFECTS TYPES OF SYMPATHETIC (ADRENERGIC) RECEPTOR PARASYMPATHETIC (CHOUNERGiq EFFECTS... 

Of the following structures, which does not respond to i-adrenergic receptor stimulation ... 

The goal of treatment of SUI is to improve urethral closure by stimulating a-adrenergic receptors in the smooth muscle of the bladder neck and proximal urethra, enhancing supportive structures underlying the urethral epithelium, or enhancing serotonin and norepinephrine effects in the micturition reflex pathways. 

Some failures will be due to the presence of variants in drug handling. Patients who are rapid acetylators of isoniazid have a slower antituberculous response than slow acetylators (Evans and Clarke, 1961). Asthmatics who do not respond well to (32-agonist bronchodilators may have fewer functioning p2-adrenergic receptors (Drysdale et al., 2000). Variations in the synthesis or structure of the serotonin transporter protein, which is involved in selective reuptake of serotonin by presynaptic neurons, may explain why some patients with depressive disorders respond to selective serotonin reuptake inhibitors and others do not (Steimer et al., 2001). 

Gouldson, P R., Snell, C. R., and Reynolds, C. A. (1997) A new approach to docking in the beta 2-adrenergic receptor that exploits the domain structure of G protein-coupled receptors. J. Med. Chem. 40, 3871-3886. 

Scheme 6.1 Chemical structures of adrenergic receptor antagonists for generation of antitarget pharmacophores class I (a) and class II (b).

Graham, R.M., Perez, D.M., Hwa, J. and Piascik, M.T. (1996) Alpha 1-adrenergic receptor subtypes. Molecular structure, function, and signaling. Circulation Research, 78, 737-749. 

De Benedetti, P.G., Cocchi, M., Menziani, M.C. and Fanelli, F. (1994) Theoretical quantitative size and shape activity and selectivity analyses of 5-HT1A serotonin and a-adrenergic receptor ligands. Journal of Molecular Structure (Theochem), 305, 101-110. 

Menziani, M.C., Montorsi, M., De Benedetti, P.G. and Karelson, M. (1999) Relevance of theoretical molecular descriptors in quantitative structure-activity relationship analysis of alphal-adrenergic receptor antagonists. Bioorganic el Medicinal Chemistry, 7, 2437-2451. 

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