(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
A series of compounds having a piperazine moiety variously linked to the benzothiazine nucleus were synthesized and evaluated for their in vitro alpha-adrenoceptor affinity by radioligand receptor binding assays. Some compounds bearing a oxyalkyl-(2-methoxyphenyl)piperazine side chain were good alpha1-adrenoreceptor ligands.
Cecchetti
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V
Istituto di Chimica e Tecnologia del Farmaco, Università di Perugia, Italy. viola@ruflo.chimfarm.unipg.it
Schiaffella
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F
Tabarrini
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Fravolini
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A
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001923:Brain Chemistry / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D066298:In Vitro Techniques; D008024:Ligands; D008168:Lung / Q000187:drug effects / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D009206:Myocardium / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects; D018341:Receptors, Adrenergic, alpha-2 / Q000187:drug effects; D018342:Receptors, Adrenergic, beta-1 / Q000187:drug effects; D018343:Receptors, Adrenergic, beta-2 / Q000187:drug effects; D013843:Thiazines / Q000138:chemical synthesis* / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D008024:Ligands; D010879:Piperazines; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; D018342:Receptors, Adrenergic, beta-1; D018343:Receptors, Adrenergic, beta-2; D013843:Thiazines