3 Adrenergic receptor antagonist pharmacological properties

PM Lish, JH Weikel, KW Dungan. Pharmacological and toxicological properties of two new (3-adrenergic receptor antagonists. J Pharmacol Exp Ther 149 161-173, 1965. 

Murmann, W., Rumore, G. and Gamba, A. (1967) Pharmacological properties of l-(4 -nitrophenyl)-2-isopropylamino-ethanol (INPEA), a new beta-adrenergic receptor antagonist. V. Effects of the optical isomers D(minus) and L(plus) INPEA on heart rate, oxygen consumption and body temperature and on the cardiac and metabolic effects of adrenaline and noradrenaline in urethane-anesthetized rats. Boll. Chim. Farm., 106, 251-268. 

Controversy surrounds the selection of a P-blocker for HF management. First, although metoprolol and carvedilol are the most commonly used p-antagonists in HF, it remains controversial as to whether one agent should be considered first-line. Carvedilol exhibits several pharmacologic properties that theoretically would confer superior efficacy, since carvedilol (1) provides blockade at multiple adrenergic receptors, which... 

Understanding the pharmacological properties of sympathomimetics and their antagonists depends on knowledge of the classification, distribution, and mechanism of action of a and fi adrenergic receptors (see Tables 6-1, 6-6, 6-7, Figure 10-1, and Table 10-6). 

PHARMACOLOGICAL EFFECTS The fi blockers vary in their lipid solubility, selectivity for the /Ij adrenergic receptor subtype, presence of partial agonist or intrinsic sympathomimetic activity, and membrane-stabilizing properties. While all of the P receptor antagonists are effective... 

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