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The synthesis of a series of N2-[4-[(arylmethyl)amino]-2, 6-dichlorophenyl]-N1,N1-dimethylformamidines that caused marked blood pressure lowering and/or diuresis in spontaneously hypertensive rats (SHR) is reported. Diuretic activity was not always associated with acute antihypertensive activity. Central nervous system effects, most notably sedation, were observed. Compound 9d, which lowered arterial blood pressure 37 mmHg in SHR when dosed at 100 mg/kg, was further evaluated in chronic hypertensive dogs because of apparent minimal CNS effects. A reduction in arterial blood pressure of 32 mmHg at 1.0 mg/kg during a 6-h postdosing interval was observed. This response was unrelated to alpha- or beta-adrenergic blockade, angiotensin I antagonism, or neuronal or ganglionic blockade. CNS effects were also observed.
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
November 1977,
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W E Meyer, and
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J E Emma
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W E Meyer, and
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Nihon rinsho. Japanese journal of clinical medicine,
W E Meyer, and
A S Tomcufcik, and
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Acta crystallographica. Section C, Crystal structure communications,
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
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Il Farmaco; edizione scientifica,
W E Meyer, and
A S Tomcufcik, and
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J E Emma
January 2006,
Bioorganic & medicinal chemistry,
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
September 2004,
Acta crystallographica. Section C, Crystal structure communications,
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
January 2004,
Acta crystallographica. Section C, Crystal structure communications,
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
June 1980,
Journal of medicinal chemistry,
W E Meyer, and
A S Tomcufcik, and
P S Chan, and
J E Emma
January 1992,
Acta pharmaceutica Nordica,
