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N, N-Diethylaminoethyl ester and 3-quinuclidinyl ester of 2, 2-diphenylpropanoic acid (compound 1 and 2, respectively) were prepared and pharmacologically evaluated in vitro and in the intact animal. Both compounds attenuated the effects of increasing doses of ACh in the isolated rat ileum (pA2 = 8.40 and 8.55, respectively). These effects were comparable to that of atropine (pA2 = 8.73). The duration of methacholine-induced salivation in male Swiss-Webster mice was significantly decreased by compound 2 but not by compound 1. Cardiorespiratory studies in adult male Sprague-Dawley rats revealed that both compounds shifted the dose-response curves to methacholine in terms of arterial blood pressure, heart rate and respiration upwards; indicative of cholinergic blockade. The observed pharmacological differences between the two compounds may be attributed to apparent in vivo hydrolysis of compound 1 by esterases.
E B Thompson, and
L B Shih, and
L Wu, and
M T Flavin, and
M C Lu
January 1956,
Farmakologiia i toksikologiia,
E B Thompson, and
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January 1964,
Acta poloniae pharmaceutica,
E B Thompson, and
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January 1959,
Farmakologiia i toksikologiia,
E B Thompson, and
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January 1979,
Acta poloniae pharmaceutica,
E B Thompson, and
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October 1968,
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E B Thompson, and
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January 1985,
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E B Thompson, and
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January 1972,
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E B Thompson, and
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June 1997,
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E B Thompson, and
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Zeitschrift fur Naturforschung. Teil B, Chemie, Biochemie, Biophysik, Biologie und verwandte Gebiete,
E B Thompson, and
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June 1974,
Bollettino chimico farmaceutico,
