5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug.
Naftopidil, a novel antihypertensive compound, possesses 5-HT1A agonistic properties in addition to being an alpha 1-adrenoceptor antagonist. The IC50 values for alpha 1-adrenoceptors (235 nmol/l) and for 5-HT1A receptors (108 nmol/l) lie in the same concentration range. The reduction in blood pressure of anesthetized cats by 8-OH-DPAT and urapidil was completely abolished by spiroxatrine, a 5-HT1A antagonist. However, the decreases in blood pressure induced by naftopidil were only partly antagonized by spiroxatrine.
Borbe
H O
HO
ASTA Pharma AG, Department of Biochemistry, Frankfurt/Main, F.R.G.
Metzenauer
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P
Szelenyi
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D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D002415:Cats; D004146:Dioxanes / Q000494:pharmacology; D018492:Dopamine Antagonists; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D010879:Piperazines / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects*; D013141:Spiro Compounds / Q000494:pharmacology; D013764:Tetrahydronaphthalenes / Q000378:metabolism
D000959:Antihypertensive Agents; D004146:Dioxanes; D018492:Dopamine Antagonists; D009281:Naphthalenes; D010879:Piperazines; D011985:Receptors, Serotonin; D013141:Spiro Compounds; D013764:Tetrahydronaphthalenes; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; C018387:spiroxatrine; C064357:naftopidil