Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta.
Characterization of alpha1-adrenoceptor-mediated contraction in the mouse thoracic aorta.
复制标题
小鼠胸主动脉α1-肾上腺素受体介导的收缩的表征。
DOI：
10.1016/s0014-2999(01)01134-7
复制
发表时间：
2001
影响因子：
5
通讯作者：
K. Koike
中科院分区：
文献类型：
--
作者：
Y. Yamamoto;K. Koike
在小鼠胸主动脉中，去甲肾上腺素、肾上腺素、苯肾上腺素和甲氧胺表现为完全激动剂。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）对每种激动剂的pA 2值与公认的α 1D-肾上腺素受体亲和力值一致。5-甲基乌拉地尔、2-[2，6-二甲氧基苯氧基乙基]氨甲基-1，4-苯并二氧六环盐酸盐（WB 4101）和哌唑嗪抑制去甲肾上腺素引起的收缩反应。小鼠胸主动脉的拮抗剂亲和力与大鼠胸主动脉天然α 1D受体或克隆α 1D受体的亲和力有显著相关性，但与α1a受体或α 1b受体的亲和力无相关性。丁螺环酮在小鼠胸主动脉中表现为部分激动剂，其收缩被BMY 7378拮抗，其pA 2值（8.49）与对去甲肾上腺素的结果（8.43）一致。可乐定为部分激动剂（pD ~ 2 =5.94）。可乐定对去甲肾上腺素的pKp值与可乐定的pD 2值相似。BMY 7378对可乐定的表观pKB值与本研究中使用的其他完全激动剂的pA 2值相似。上述结果表明，小鼠胸主动脉存在α 1D肾上腺素受体亚型，完全激动剂和部分激动剂均通过α 1D肾上腺素受体介导引起收缩。
In the mouse thoracic aorta, noradrenaline, adrenaline, phenylephrine and methoxamine behaved as full agonists. The pA2values for 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4,5]decane-7,9-dione dihydrochloride (BMY 7378) against each agonist were in good agreement with the generally accepted affinity value of α1D-adrenoceptors. 5-Methylurapidil, 2-[2,6-dimethoxyphenoxyethyl]aminomethyl-1,4-benzodioxane hydrochloride (WB 4101) and prazosin inhibited the contraction in response to noradrenaline. A significant correlation was obtained between the antagonist affinities in mouse thoracic aorta and those of native α1D-adrenoceptors in rat thoracic aorta or with those of cloned α1d-adrenoceptors, but not with those for either α1a- or α1b-adrenoceptors. Buspirone behaved as a partial agonist in mouse thoracic aorta, the contraction of which was antagonized by BMY 7378 with a pA2value (8.49) consistent with that found against noradrenaline (8.43). Clonidine acted as a partial agonist (pD2=5.94). The pKpvalue for clonidine against noradrenaline was similar to the pD2value for clonidine. The apparent pKBvalue for BMY 7378 against clonidine was similar to the pA2value against other full agonists used in the present study. These results suggest that the α1D-adrenoceptor subtype exists, and that the full agonists and the partial agonists evoke the contraction mediated through the α1D-adrenoceptor in mouse thoracic aorta.
α 1-肾上腺素能受体亚型、磷酸肌醇和细胞 Ca2 来源。
影响因子：
21.1
作者：
Minneman,KP
通讯作者：
Minneman,KP
编码小鼠 α2c-肾上腺素受体同系物的基因的靶向失活。
DOI：
--
发表时间：
1995
期刊：
Molecular pharmacology.
影响因子：
--
作者：
Link,RE;Stevens,MS;Kulatunga,M;Scheinin,M;Barsh,GS;Kobilka,BK
通讯作者：
Kobilka,BK
影响因子：
3.6
作者：
C. Forray;J. Bard;J. Wetzel;G. Chiu;E. Shapiro;R. Tang;H. Lepor;P. Hartig;R. Weinshank;T. Branchek
通讯作者：
C. Forray;J. Bard;J. Wetzel;G. Chiu;E. Shapiro;R. Tang;H. Lepor;P. Hartig;R. Weinshank;T. Branchek