Different effects of serotonin antagonists on 3H-mianserin and 3H-ketanserin recognition sites.

Different effects of serotonin antagonists on 3H-mianserin and 3H-ketanserin recognition sites.
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血清素拮抗剂对 3H-米安色林和 3H-酮色林识别位点的不同作用。

DOI:
10.1016/0024-3205(85)90190-0
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发表时间:
1985
期刊:
影响因子:
6.1
通讯作者:
E. Costa
E. Costa
中科院分区:
医学2区
文献类型:
--
作者:
O. Gandolfi;M. Barbaccia;E. Costa

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在用酮色林(10 mg/kg i. p.)或米安色林(5 mg/kg i. p.)每天两次,持续21天,NE(100 μM)刺激的腺苷酸环化酶的Vmax减弱,表明酮色林和米安色林与许多抗抑郁药一样具有减弱NE刺激的腺苷酸环化酶的能力。按上述给药方案连续给药7天,可使5 HT 2识别位点的Bmax降低,但对3 H-米安色林结合的Bmax和表观Kd均无影响。单次注射米安色林也可引起5 HT 2结合位点的Bmax显著降低(1)。这种药物也下调其自身的结合时,每天两次给药3周。根据该信息和其他信息(2,3),可以得出结论,酮色林和米安色林与不同的识别位点结合。5-HT 2和米安色林识别位点在功能上可能相关,并且多巴胺能突触可能受到多种化学信号的调节。
In minces prepared from the frontal cortex of rats treated with ketanserin (10 mg/kg i.p.) or mianserin (5 mg/kg i.p.) twice daily for 21 days, the Vmax of the adenylate cyclase stimulated by NE (100 μM) is attenuated, suggesting that ketanserin and mianserin share with a number of antidepressants the ability to attenuate the adenylate cyclase stimulation by NE. Ketanserin, given with the above mentioned dose schedule for 7 consecutive days, reduced the Bmax of 5HT2recognition sites but failed to change either the Bmax or the apparent Kd of3H-mianserin binding. A significant decrease in the Bmax of 5HT2binding sites is elicited also by a single injection of mianserin (1). This drug also down-regulates its own binding when given twice daily for 3 weeks. From this and other information (2,3), it is concluded that ketanserin and mianserin bind to distinct recognition sites. The possibility that 5HT2and mianserin recognition sites are functionally related and that serotonergic synapses are modulated by multiple chemical signals might be considered.
长期抗抑郁药治疗会降低螺哌啶醇标记的血清素受体结合。
DOI: 10.1126/science.6251550
发表时间: 1980
期刊: Science (New York, N.Y.)
影响因子: --
作者:
Peroutka,SJ;Snyder,SH
通讯作者: Snyder,SH
米安色林急性和慢性治疗后血清素受体敏感性。
DOI: --
发表时间: 1982
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Blackshear,MA;Sanders-Bush,E
通讯作者: Sanders-Bush,E
[3H]Mianserin:大鼠脑中血清素和组胺受体的差异标记。
DOI: --
发表时间: 1981
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
Peroutka,SJ;Snyder,SH
通讯作者: Snyder,SH