Al-adrenergic receptors

Montorsi, M., Menziani, M.C., Cocchi, M., Fanelli, F. and De Benedetti, P.G. (1998) Computer modeling of size and shape descriptors of al-adrenergic receptor antagonists and quantitative structure-affinity / selectivity relationships. Methods, 14, 239-254. 

Bonaventure P, Nepomuceno D, Hein L, Sutcliffe JG, Lovenbeig T, Hedlund PB. Radioligand binding analysis of knockout mice reveals 5-hydroxytryptamine7 receptor distribution and uncovers 8-hydroxy-2-(di- -propylamino)tetralin interaction with al adrenergic receptors. Neuroscience 2004 124 901-911. 

Hu LA, Tang Y, Miller WE, et al. -Adrenergic receptor association with PSD-95. Inhibition of receptor internalization and facilitation of pradrenergic receptor interaction with -mcthyl-D-aspartatc receptors. J Biol Chem 2000 275 38,659-38,666. 

Hwa J, Perez DM. The unique nature of the serine interactions for al-adrenergic receptor agonist binding and activation. J Biol Chem 1996 271(ll) 6322-6327. 

Muscarinic acetylcholine-receptor hgand, al-Adrenergic-receptor (IC50 = 1 gM),... 

Risperidone (11) was also included among a al-adrenergic receptor antagonists to study a quantitative structure activity relationship (99BMC2437). A pharmacophore model for atypical antipsychotics, including 11, was established (00MI4I). An increased plasma level of 11 and 9-hydroxyrisperidone (12) was observed in combination with paroxetine (01 Mil 3). The effect of vanlafaxine on the pharmacokinetics of 11 was reported (99MII3). 

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... 

Rochais F, Vilardaga JP, Nikolaev VO et al (2007) Realtime optical recording of Pi-adrenergic receptor activation reveals supersensitivity of the Arg389 variant to carvedi-lol. J Clin Invest 117229-235... 

Hnggett, D.B., Brooks, B.W., and Peterson, B. et al. (2002). Toxicity of select beta adrenergic receptor blocking pharmaceuticals (beta blockers) on aqnatic organisms. Archives Environmental Contamination and Toxicology 41, 229-235. 

Fig. 5.12 (a) Synaptic types along dendritic spines of M/T and GC units uni-, and bi-directional junctions, (b) Transmitter systems at a reciprocal synapse, Mitral-Granule cell junction. [Glu, glutamate (R, receptor) GABA, y-aminobutyric acid (R, receptor) E, intracellular effector and aAR, alpha-adrenergic receptor.]. (From Hayashi et al., 1993.)... 

Ballesteros JA, Jensen AD, Liapakis G, et al. Activation of the beta 2-adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6. J Biol Chem 2001 276(31) 29171-29177. 

McGraw DW, Mihlbachler KA, Schwarb MR, et al. Airway smooth muscle prostaglandin-EPl receptors directly modulate beta2-adrenergic receptors within a unique heterodimeric complex. J Clin Invest 2006 116 1400-1409. 

Wilson AL, Womble SW, Prakash C, Cragoe EJ Jr, Blair IA, Limbird LE. Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+ /H exchange. Mol Pharmacol 1992 42 175-179. 

Drysdale CM, McGraw DW, Stack CB, Stephens JC, Judson RS, Nandabalan K et al. Complex promoter and coding region 2-adrenergic receptor haplotypes alter receptor expression and predict in... 

Holloway JW, Dunbar PR, Riley GA, Sawyer GM, Fitzharris PF, Pearce N et al. Association of beta2-adrenergic receptor polymorphisms with severe asthma. Clin Exp Allergy 2000 30[8] 1097-1103. 

McGraw DW, Forbes SL, Kramer LA et al. Transgenic overexpression of beta[2]-adrenergic receptors in airway smooth muscle alters myocyte function and ablates bronchial hyperreactivity. J Biol Chem 1999 274 32241-32247. 

Israel E, Drazen JM, Liggett SB et al. The effect of polymorphisms of the beta[2]-adrenergic receptor on the response to regular use of albuterol in asthma. Am J Respir Crit Care Med 2000 162 75-80. 

Weir TD, Mallek N, Sandford AJ et al. y82-Adrenergic receptor haplotypes in mild, moderate and fatal/near fatal asthma. Am J Respir Crit Care Med 1998 158 787-791. 

Drysdale, C.M., et al., "Complex Promoter and Coding Region Beta 2-Adrenergic Receptor Haplotypes Alter Receptor Expression and Predict in Vivo Responsiveness," Proc. Natl. Acad. Sci. U.S.A., 97, 10483-10488 (2000). 

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). 

Sufficient data were not included in other reports to calculate predictive values. For instance, Drysdale et al. (2000) reported over a twofold difference between responses to bronchodilators in asthmatics who differed in haplotypes of the [1,-adrenergic receptor gene, but predictive values could not be calculated because the number of asthmatics in each response and haplo-type category were not given. Marked differences in mean absorption of digoxin between indi-... 

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