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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Walduck, K. O'donnell, S. R. Wanstall, J. C. |
| Abstract | 1 PA2 values for beta-adrenoceptor antagonists were obtained on isolated preparations of guinea-pig trachea (intrinsic tone) and atria (rate), with isoprenaline, noradrenaline (beta 1-selective) and fenoterol (beta 2-selective) as agonists. Uptake mechanisms and alpha-adrenoceptors were inhibited. The antagonists studied were (+/-)-threo-alpha-methylpropranolol. (+/-)-1(4-benzimidazoloxy)-3-isopropylamino-2-propanol (4-BIP) and (+/-)-1-(5-benzimidazoloxy)-3-isopropylamino-2-propanol (5-BIP). 2 4-BIP was a potent beta-adrenoceptor antagonist but it was not selective for trachea (pA2 on trachea 7.88 and on atria 7.73, fenoterol as agonist). 5-BIP was less than one tenth as active as 4-BIP and was therefore not studied in detail. 3 alpha-Methylpropranolol was potent and it was also selective for trachea (pA2 on trachea 8.24 and on atria 7.56, fenoterol as agonist). This selectivity was not seen with isoprenaline as agonist. In tracheal preparations contracted by carbachol the slope of the Schild plot for alpha-methylpropranolol was less than 1.0 (isoprenaline as agonist). 4 alpha-Methylpropranolol, although not highly selective for beta 2-adrenoceptors, is considerably more potent than the alternative beta 2-selective antagonists available at present. Therefore, it may be useful in studies designed to classify beta-adrenoceptor subtypes in tissues. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 4 |
| Volume Number | 68 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1980-04-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Adrenergic Beta-Antagonists Myocardial Contraction Drug Effects Propranolol Analogs & Derivatives Trachea Animals Guinea Pigs In Vitro Techniques Muscle Contraction Organ Specificity Phenoxybenzamine Pharmacology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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