Abstract
A recent uroselective alpha(1)-adrenoceptor antagonist, REC15/2739, has been joined with nitrooxy and furoxan NO-donor moieties to give new NO-donor alpha(1)-antagonists. All the compounds studied proved to be potent and selective ligands of human cloned alpha(1a)-receptor subtype. Derivatives 6 and 7 were able to relax the prostatic portion of rat vas deferens contracted by (-)-noradrenaline because of both their alpha(1A)-antagonist and their NO-donor properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-Antagonists / chemical synthesis
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / pharmacology
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Animals
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Binding, Competitive
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CHO Cells
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Chromones / chemical synthesis*
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Chromones / chemistry
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Chromones / pharmacology
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Cricetinae
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HeLa Cells
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Humans
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In Vitro Techniques
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Male
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Muscle Relaxation
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Muscle, Smooth / drug effects
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Muscle, Smooth / physiology
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Nitric Oxide Donors / chemical synthesis*
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Nitric Oxide Donors / chemistry
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Nitric Oxide Donors / pharmacology
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Nitrous Acid / chemistry*
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Oxadiazoles / chemical synthesis*
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Oxadiazoles / chemistry
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Oxadiazoles / pharmacology
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Radioligand Assay
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Rats
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Receptors, Adrenergic, alpha-1 / drug effects
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Adrenergic, alpha-2 / drug effects
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Receptors, Adrenergic, alpha-2 / metabolism
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism
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Receptors, Serotonin, 5-HT1
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Vas Deferens / drug effects
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Vas Deferens / physiology
Substances
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ADRA1A protein, human
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Adra1a protein, rat
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Adrenergic alpha-Antagonists
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Chromones
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Nitric Oxide Donors
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Oxadiazoles
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Rec 15-2739
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Receptors, Adrenergic, alpha-1
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Receptors, Adrenergic, alpha-2
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Receptors, Serotonin
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Receptors, Serotonin, 5-HT1
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furoxans
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Nitrous Acid