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Methoctramine selectively blocks cardiac muscarinic M2 receptors in vivo (1988)

Wess, Jürgen ; Angel, Piero ; Melchiorre, Carlo ; [et al.]

Springer

Naunyn-Schmiedeberg's archives of pharmacology 338 (1988), S. 246-249

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ISSN: 1432-1912

Keywords: Methoctramine ; Polymethylene tetraamines ; Cardioselectivity ; M1/M2 receptors ; Muscarinic receptor subtypes

Source: Springer Online Journal Archives 1860-2000

Topics: Medicine

Notes: Summary The antimuscarinic effects of methoctramine (N, N′- bis[6-[(2-methoxybenzyl)amino]hexyl]-1,8-octanediamine tetrahydrochloride), a polymethylene tetraamine endowed with high cardioselectivity in vitro, were assessed in two in vivo preparations. Methoctramine (300 μg/kg i.v.) strongly inhibited the methacholine- and muscarine-induced bradycardia in the anaesthetized and pithed rat, respectively. The same dose of methoctramine did not significantly affect the depressor action of methacholine in the anaesthetized rat mediated by vascular M2 receptors. Furthermore, even high doses of methoctramine (up to 1 mg/kg i. v.) did not reduce the ganglionic M1 receptor-mediated tachycardia and pressor response to muscarine or McN-A-343 in the pithed rat. These data suggest that methoctramine while showing high affinity for cardiac M2α receptors has rather low affinity for ganglionic M1 and vascular M2 receptors. This in vivo study thus provides further evidence to support the view that methoctramine is a potent and highly selective antagonist of cardiac M2α receptors.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00173395

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Stereoselectivity at muscarinic receptor subtypes: observations with the enantiomers of phenglutarimide (1989)

Lambrecht, Günter ; Feifel, Roland ; Mutschler, Ernst

New York, NY [u.a.] : Wiley-Blackwell

Chirality 1 (1989), S. 170-173

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ISSN: 0899-0042

Keywords: phenglutarimide enantiomers ; enantioselectivity ; antiparkinsonian drugs ; M1-selective antagonists ; rabbit vas deferens ; pirenzepine ; Chemistry ; Organic Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Notes: The affinity of the enantiomers of phenglutarimide at three muscarinic receptor subtypes was examined in vitro using field-stimulated rabbit vas deferens (M1 receptors) and guinea pig atria (M2α receptors) and ileum (M2β receptors). Extremely high stereoselectivity was observed and higher affinities (up to 6000-fold) were found for the (+)-S-enantiomer. The stereoselectivity ratios were different at the three subtypes, and the stereochemical demands made by the muscarinic receptors were most stringent at M1 receptors. (+)-(S)-Phenglutarimide was found to be a potent M1-selective antagonist (pA2 at M1 = 8.53). Its receptor selectivity profile is qualitatively similar to that of pirenzepine. (-)-(R)-Phenglutarimide showed no comparable discriminatory properties.

Additional Material: 1 Ill.