By D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)
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Extra info for Adrenergic Activators and Inhibitors: Part I
Removal of the p-hydroxyl caused a greater decrease of p-stimulant properties than of ex-stimulant properties (TRIGGLE and TRIGGLE, 1976). A more detailed description of the effect of substituent variations of the catecholamine structure on ex(and p)-receptor activities can be found in TRIGGLE (1970) and AVIADO (1970). Cl H Q-N~) Cl (120) (121) (122) (123) The imidazolines were first investigated by HARTMANN and ISLER in 1939 (see also CAVALLINI et at, 1959). This work led to the introduction of two clinically useful drugs, naphazoline (120), an ex-adrenergic stimulant that found use as a nasal decongestant, and tolazoline (6), an ex-adrenergic blocker with antihypertensive properties but which also causes heart stimulation and is now used as a vasodilator.
6,7-Dihydroxytetrahydroisoquinoline (54), an analog of the cis, fJ-rotamer of dopamine, did not increase renal blood flow. Compound (52) and isoproterenol pro- 15 Chemistry of Alpha- and Beta-Adrenoceptor Agonists and Antagonists duced pronounced and similar increases of canine femoral blood flow, which was blocked by propranolol. Both compound (53) and dopamine produced insignificant changes in femoral blood flow. trans, ~-rotamer trans, ()(-rotamer (49) cis, ~-rotamer (51) (50) OH HO~ HO~ HO~I)'H H~NH2 ~NH2 (52) H~ (54) (53) This work supports the premise that the trans, p-rotamer of dopamine is important in receptor recognition of the dopaminergic receptor, and the trans, (X-rotamer is important at p-receptors.
1974). b) 3,5-Dihydroxy Substitution (Resorcinols) Removal of either hydroxyl group of isoproterenol yielded compounds with little or no p-stimulant properties (LANDS and BROWN, 1967). , 1961). However, it had a longer duration of action and was 50 times more potent than isoproterenol by oral administration. It also showed significant P2-selectivity. , terbutaline (37) and fenoterol (25) (O'DONNELL and WANSTALL, 1974). , 1977) diminished or eliminated p-agonist activity. c) Nonphenolic Phenylethanolamines A small number of compounds have been found that produce direct stimulation of the p-adrenoceptors and yet have no phenolic groups on the aromatic ring.