5-羟色胺1B受体和α2A/2C肾上腺素能受体介导二氢麦角胺引起的颈外血管收缩。
5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine.
作者信息
Villalón Carlos M, Centurión David, Willems Edwin W, Arulmani Udayasankar, Saxena Pramod R, Valdivia Luis F
机构信息
Departamento de Farmacobiología, CINVESTAV-IPN, Calzada de los Tenorios 235, Col. Granjas Coapa, Deleg. Tlalpan, C.P. 14330 México, D.F., Mexico.
出版信息
Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90. doi: 10.1016/j.ejphar.2003.11.026.
Dihydroergotamine produces external carotid vasoconstriction in vagosympathectomized dogs by 5-HT(1B/1D) receptors and alpha(2)-adrenoceptors. This study identified the specific subtypes involved in this response. One-minute intracarotid infusions of dihydroergotamine (5.6-10 microg/min) dose-dependently decreased external carotid blood flow without affecting blood pressure or heart rate. This response was: (1) partly blocked in dogs pretreated intravenously with the antagonists SB224289 (5-HT(1B); 2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4' (5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carbonyl]furo[2,3-f]indole-3-spiro-4'-piperidine hydrochloride), rauwolscine (alpha(2)), BRL44408 (alpha(2A); 2-[2H-(1-methyl-1,3-dihydroisoindole)methyl]-4,5-dihydroimidazole) or MK912 (alpha(2C); (2S,12bS)-1'3'-dimethylspiro(1,3,4,5',6,6',7,12b-octahydro-2Hbenzo[b]furo[2,3-a]quinazoline)-2,4'-pyrimidin-2'-one); (2) markedly blocked after SB224289 plus rauwolscine; and (3) unaffected after BRL15572 (5-HT(1D); 1-(3-chlorophenyl)-4-[3,3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride) or imiloxan (alpha(2B)). Therefore, the above response involves 5-HT(1B) receptors and alpha(2A/2C)-adrenoceptors.
双氢麦角胺通过5-HT(1B/1D)受体和α(2)-肾上腺素能受体使去迷走交感神经犬的颈外血管收缩。本研究确定了参与该反应的具体亚型。颈内动脉内输注双氢麦角胺（5.6 - 10微克/分钟）1分钟，剂量依赖性地降低颈外血流，而不影响血压或心率。该反应：(1) 在用拮抗剂SB224289（5-HT(1B)；2,3,6,7-四氢-1'-甲基-5-[2'-甲基-4'-(5-甲基-1,2,4-恶二唑-3-基)联苯-4-羰基]呋喃并[2,3-f]吲哚-3-螺-4'-哌啶盐酸盐）、萝芙辛（α(2)）、BRL44408（α(2A)；2-[2H-(1-甲基-1,3-二氢异吲哚)甲基]-4,5-二氢咪唑）或MK912（α(2C)；(2S,12bS)-1'3'-二甲基螺(1,3,4,5',6,6',7,12b-八氢-2H-苯并[b]呋喃并[2,3-a]喹唑啉)-2,4'-嘧啶-2'-酮）静脉预处理的犬中部分被阻断；(2) 在SB224289加萝芙辛后明显被阻断；(3) 在BRL15572（5-HT(1D)；1-(3-氯苯基)-4-[3,3-二苯基(2-(S,R)羟基丙基)哌嗪]盐酸盐）或咪洛克生（α(2B)）后不受影响。因此，上述反应涉及5-HT(1B)受体和α(2A/2C)-肾上腺素能受体。
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