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D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)'s Adrenergic Activators and Inhibitors: Part I PDF

By D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)

ISBN-10: 3642675050

ISBN-13: 9783642675058

ISBN-10: 3642675077

ISBN-13: 9783642675072

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Extra resources for Adrenergic Activators and Inhibitors: Part I

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1974). Both aromatic ring substituents and amine substituents are important. , 1976). However, penetration into the central nervous system is probably dependent on lipophilicity and therefore, the greater the membrane stabilizing activity (m. s. ) the greater the likelihood of penetration into the central nervous system. D. Alpha-Adrenergic Agonists The a-adrenergic agonists, as defined classically (AHLQUIST, 1948, 1966), cause vasoconstriction of vascular smooth muscle and contraction of spleen muscle, of the seminal vesicles, of the dog retractor penis, of the uterus, and of the nictitating membrane.

Was eliminated. a. Replacement of an isopropyl by an N-aryloxyethyl group as in tolamolol (93) can eliminate agonist activity (CLARKSON, 1976). Agonist properties can be introduced into the molecule. Hydroxybenzylpropranolol (92) has substantial agonist properties; propranolol does not (Y AMAMURA and RODBELL, 1976). Hydroxybenzylpindolol (66) is both a potent antagonist and a potent partial agonist, having a higher affinity for Chemistry of Alpha- and Beta-Adrenoceptor Agonists and Antagonists 27 the {:1-receptor than isoproterenol.

H 20 # ~ -C(CH'>. h 15-20 ....... 1 OCH 2- 'Q CH,s02NH ....... l lvN)-(,OCH,- I I -CH(CH'>2 -C(CH'>. N CH,cONH'U Practolol ....... OCH,CH''U Metoprolol ....... OCH,CH,0'U H87/07 ....... 1 + + OCH,- H,NCOCH,'U Atenolol ....... 1 + OCH,- CH,cH,CH,CONH,((COCH. Acebutolol Tolamolol ....... ~ ....... 8 CH. • In vivo blockade of isoproterenol tachycardia (propranolol = I). b Intrinsic sympathomimetic activity. C Nonspecific membrane stabilizing activity . " Cardioselectivity relative to bronchi. , 1964) into clinical practice.

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Adrenergic Activators and Inhibitors: Part I by D. K. Phillips (auth.), Professor Dr. Lászlo Szekeres (eds.)

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