3-Adrenergic receptors pharmacological characteristics

Porter JE, Perez DM. Characteristics for a salt-bridge switch mutation of the alpha(lb) adrenergic receptor. Altered pharmacology and rescue of constitutive activity. J Biol Chem 1999 274 34,535-34,538. 

The paradigm used by Ahlquist for classifying receptors based on their pharmacological characteristics (i.e., rank order of potency of agonists) was further developed by Lands and colleagues with the subdivision of the P-adrenergic receptors into pr and P2-subtypes (12). The pradrenergic receptor, the dominant receptor in heart and adipose tissue, was equally sensitive to epinephrine and... 

Bylund DB, Blaxall HS, Iversen LJ, Caron MG, Lefkowitz RJ, Lomasney JW. Pharmacological characteristics of a2-adrenergic receptors comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol 1992 42 1-5. 

Metabolic responses in adipocytes and certain other tissues with atypical pharmacological characteristics may be mediated by this subtype of receptor. Most adrenergic receptor antagonists (including propranolol) do not block these responses. 

First, we synthesized a series of cirazoline derivatives and evaluated their pharmacological effects on rabbit aorta and their I receptor affinity on rabbit kidney membranes. The results reported in Table 1 show that their ability to interact with ai-adrenergic as opposed to I receptors follows a characteristic pattern. 

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