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β‐Adrenoceptor blocking properties and cardioselectivity of M & B 17,803A
Author(s) -
BASIL B.,
JORDAN R.,
LOVELESS A. H.,
MAXWELL D. R.
Publication year - 1973
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1973.tb06906.x
Subject(s) - practolol , propranolol , potency , bronchospasm , isoprenaline , pharmacology , guinea pig , medicine , propranolol hydrochloride , chemistry , anesthesia , endocrinology , stimulation , asthma , biochemistry , in vitro
Summary1 . The β‐adrenoceptor blocking properties of (±)‐1‐(2‐acetyl‐4‐ n ‐butyramidophenoxy)‐2‐hydroxy‐3‐isopropylaminopropane hydrochloride (M&B 17,803A) have been compared with those of practolol and propranolol in the guinea‐pig, cat and dog. 2 . Following either intravenous or oral administration in the cat or dog, M&B 17,803A and practolol had similar potency in antagonizing isoprenaline‐induced tachycardia and both showed cardioselectivity, but both were less potent than propranolol. 3 . M&B 17,803A and practolol had approximately one hundredth the intravenous potency of propranolol in increasing the severity of anaphylactic bronchospasm in the conscious sensitized guinea‐pig. 4 . M&B 17,803A possessed less marked intrinsic sympathomimetic activity than practolol but, like propranolol, it had significant local anaesthetic properties and increased the refractory period of rabbit isolated atria.