Abstract
A series of new 3-aryl-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridines was synthesized and screened for in vitro [3H]prazosin displacement activity. The results correlated well with their antihypertensive activity in spontaneous hypertensive rats. 1-Benzyl-3-(4-fluorophenyl)-4,5,6,7-tetrahydropyrazolo[4,3-c]pyrid ine (50, L 16052) was selected for further pharmacological evaluations of its potency when administered orally to conscious renal hypertensive dogs.
MeSH terms
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Animals
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Brain / metabolism
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Cats
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Chemical Phenomena
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Chemistry
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Dogs
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Hypertension / drug therapy*
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Hypertension, Renovascular / drug therapy
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Male
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Mice
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Prazosin / metabolism*
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Pyrazoles / chemical synthesis
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Pyrazoles / metabolism
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Pyrazoles / therapeutic use*
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Pyridines / chemical synthesis
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Pyridines / metabolism
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Pyridines / therapeutic use*
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Quinazolines / metabolism*
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Rats
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Receptors, Adrenergic, alpha / metabolism
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Structure-Activity Relationship
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Synaptosomes / metabolism
Substances
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Pyrazoles
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Pyridines
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Quinazolines
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Receptors, Adrenergic, alpha
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Prazosin