Beta-adrenergic-receptor agonists/antagonists

Weiland GA, Minneman KP, Molinoff PB (1979) Fundamental difference between the molecular interactions of agonists and antagonists with the beta-adrenergic receptor. Nature 281(5727) 114-117... 

Strader, C. D., Candelore, M. R., Hill, W. S., Dixon, R. A., and Sigal, I. S. (1989a). A single amino acid substitution in the beta-adrenergic receptor promotes partial agonist activity from antagonists. J. Biol. Chem. 264, 16470-16477. 

Neve K A, Molinoff PB. Effects of chronic administration of agonists and antagonists on the density of beta-adrenergic receptors. Am J Cardiol 1986 57(12) 17F-22F. 

Purse, K.E. and Lybrand, T.P. (2003) Three-dimensional models for beta-adrenergic receptor complexes with agonists and antagonists. Journal of Medicinal Chemistry, 46 (21), 4450-4462. 

Both PEA and TYR are agonists of TAARl, but PEA is more potent than TYR [18]. On the other hand, TYR and PEA are partial allosteric antagonists at beta-adrenergic receptors 1 and 2, which are highly similar to TAAR 1 [18]. 

D. Hughes, E. Grabowski, P. Reider, Practical chemoenzymatic synthesis of a pyr-idylethanolamino beta-3 adrenergic receptor antagonist - stereospecific beta-3 agonist used in obesity therapy, produced by yeast-mediated asymmetric reduction of a ketone, Tetrahedron Lett. 1999, 40 (37j, 6739-6743. 

Alpha and beta blockers compete with endogenous agonists for adrenergic receptors. Antagonist occupation of al receptors inhibits vasoconstriction and occupation of pi receptors prevents adrenergic stimulation of the heart. 

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