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对照大鼠和利血平化大鼠尾动脉近端节段中的α1-肾上腺素能受体

alpha1-Adrenoceptors in proximal segments of tail arteries from control and reserpinised rats.

作者信息

Kamikihara Susana Y, Mueller André, Lima Vanessa, Akinaga Juliana, Nojimoto Fernanda D, Castilho Anthony, Buratini José, Pupo André S

机构信息

Department of Pharmacology, Instituto de Biociências, UNESP, Botucatu, SP 18618-000, Brazil.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2007 Oct;376(1-2):117-26. doi: 10.1007/s00210-007-0176-4. Epub 2007 Aug 4.

Abstract

It has been recently shown that the supersensitivity of distal segments of the rat tail artery to phenylephrine after chemical sympathectomy with reserpine results from the appearance of alpha(1D)-adrenoceptors. It is known that both alpha(1A)- and alpha(1D)-adrenoceptors are involved in the contractions of proximal portions of the rat tail artery. Therefore, this study investigated whether sympathectomy with reserpine would induce supersensitivity in proximal segments of the rat tail artery, a tissue in which alpha(1D)-adrenoceptors are already functional. Proximal segments of tail arteries from reserpinised rats were three- to sixfold more sensitive to phenylephrine and methoxamine than were arteries from control rats (n = 6-2; p < 0.05). The imidazolines N-[5-(4,5-Dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide hydrobromide (A-61603) and oxymetazoline, which activate selectively alpha(1A)-adrenoceptors, were equipotent in tail arteries from control and reserpinised rats (n = 4-2; p < 0.05), whereas buspirone, which activates selectively alpha(1D)-adrenoceptor, was approximately 4-fold more potent in tail arteries from reserpinised rats (n = 4-6; p < 0.05). Prazosin (nonselective) and 5-methylurapidil (alpha(1A)-selective), were competitive antagonists of contractions induced by phenylephrine and were equipotent in tail arteries from control and reserpinised rats (n = 4-6). The selective alpha(1D)-adrenoceptor antagonist 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione dihydrochloride (BMY-7378) presented similar complex antagonism in tail arteries from control and reserpinised rats, with Schild slopes much lower than 1.0 (p < 0.05, n = 4-6). Semiquantitative reverse transcriptase polymerase chain reaction (RT-PCR) revealed that mRNA encoding alpha(1A)-and alpha(1B)-adrenoceptors are similarly distributed in tail arteries from control and reserpinised rats, whereas mRNA for alpha(1D)-adrenoceptors is twice more abundant in the tail artery from reserpinised rats. In conclusion, the supersensitivity induced by reserpine is related only to alpha(1D)-adrenoceptors, even in tissues where this receptor subtype is already present and functional. Only the use of subtype-selective alpha(1)-adrenoceptor agonists detected the increased alpha(1D)-adrenoceptor component after reserpinisation, as the antagonists behaved similarly in tail arteries from control and reserpinised rats.

摘要

最近研究表明,用利血平进行化学性交感神经切除术后,大鼠尾动脉远段对去氧肾上腺素的超敏感性是由α(1D)-肾上腺素能受体的出现所致。已知α(1A)-和α(1D)-肾上腺素能受体均参与大鼠尾动脉近段的收缩。因此,本研究调查了用利血平进行交感神经切除是否会在大鼠尾动脉近段诱发超敏感性,该组织中α(1D)-肾上腺素能受体已发挥功能。来自利血平处理大鼠的尾动脉近段对去氧肾上腺素和甲氧明的敏感性比对照大鼠的动脉高3至6倍(n = 6 - 2;p < 0.05)。选择性激活α(1A)-肾上腺素能受体的咪唑啉类化合物N-[5-(4,5-二氢-1H-咪唑-2-基)-2-羟基-5,6,7,8-四氢萘-1-基]甲磺酰胺氢溴酸盐(A-61603)和羟甲唑啉,在对照和利血平处理大鼠的尾动脉中效力相当(n = 4 - 2;p < 0.05),而选择性激活α(1D)-肾上腺素能受体的丁螺环酮,在利血平处理大鼠的尾动脉中的效力约高4倍(n = 4 - 6;p < 0.05)。哌唑嗪(非选择性)和5-甲基乌拉地尔(α(1A)-选择性)是去氧肾上腺素诱导收缩的竞争性拮抗剂,在对照和利血平处理大鼠的尾动脉中效力相当(n = 4 - 6)。选择性α(1D)-肾上腺素能受体拮抗剂8-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-8-氮杂螺[4.5]癸烷-7,9-二酮二盐酸盐(BMY-7378)在对照和利血平处理大鼠的尾动脉中表现出类似的复杂拮抗作用,其希尔德斜率远低于1.0(p < 0.05,n = 4 - 6)。半定量逆转录酶聚合酶链反应(RT-PCR)显示,编码α(1A)-和α(1B)-肾上腺素能受体的mRNA在对照和利血平处理大鼠的尾动脉中分布相似,而α(1D)-肾上腺素能受体的mRNA在利血平处理大鼠的尾动脉中丰度高出两倍。总之,利血平诱导的超敏感性仅与α(1D)-肾上腺素能受体有关,即使在该受体亚型已经存在并发挥功能的组织中也是如此。只有使用亚型选择性α(1)-肾上腺素能受体激动剂才能检测到利血平处理后α(1D)-肾上腺素能受体成分的增加,因为拮抗剂在对照和利血平处理大鼠的尾动脉中表现相似。

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