5-Hydroxytryptamine receptor agonists influence calcium-stimulated adenylate cyclase activity in the cerebral cortex and hippocampus of the rat.

5-Hydroxytryptamine receptor agonists influence calcium-stimulated adenylate cyclase activity in the cerebral cortex and hippocampus of the rat.
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5-羟色胺受体激动剂影响大鼠大脑皮层和海马中钙刺激的腺苷酸环化酶活性。

DOI:
10.1016/0014-2999(90)90560-s
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发表时间:
1990
影响因子:
5
通讯作者:
A. Geisler
A. Geisler
中科院分区:
医学2区
文献类型:
--
作者:
A. Mørk;A. Geisler

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本文研究了5-羟色胺(5-HT)受体激动剂对钙(Ca ~(2+))刺激的大鼠海马和大脑皮层腺苷酸环化酶活性的影响。在Ca 2+(1.5 μM)存在下,5-HT剂量依赖性地抑制腺苷酸环化酶活性(EC 50 = 10 ± 2 nM)。5-HT对Ca ~(2+)刺激的腺苷酸环化酶的抑制作用可被螺哌隆(KB= 2 ± 0.8 nM)拮抗。5-HT激动剂抑制海马腺苷酸环化酶活性的顺序为:5-羧酰胺色胺(5-CT)> 8-羟基-2-(二正丙基氨基)四氢萘(8-OH-DPAT)> 5-羟色胺(5-HT)= 5-甲氧基色胺(5-OCH 3-T)>三氟甲基苯基哌嗪(TFMPP)>间氯苯基哌嗪(mCPP)。2-甲基-5-羟色胺(2-CH_3 -5-HT)对Ca ~(2+)刺激的酶活性无影响。在无Ca ~(2+)时,5-HT对大脑皮层腺苷酸环化酶活性有双相刺激作用(EC_(50)= 0.2 ± 0.04 nM和10 ± 3μM),而8-OH-DPAT、5-CT和2-CH_3 -5-HT对腺苷酸环化酶活性有双相刺激作用。在Ca ~(2+)(1.5 μM)存在下,低浓度的5-HT、8-OH-DPAT、5-CT和2-CH_3 -5-HT可增强腺苷酸环化酶的活性,而高浓度的5-HT、8-OH-DPAT、5-CT和2-CH_3 - 5-HT则抑制腺苷酸环化酶的活性。我们建议,5-HT受体介导的抑制钙刺激腺苷酸环化酶在大鼠海马对应于5-HT 1A亚型。5-HT似乎通过非典型的5-HT受体增强Ca ~(2+)刺激的大脑皮层腺苷酸环化酶活性,并通过5-HT_(1A)受体降低酶活性。
The effects of 5-hydroxytryptamine (5-HT) receptor agonists on calcium (Ca2+)-stimulated adenylate cyclase activity in the hippocampus and cerebral cortex of the rat were studied. In the presence of Ca2+(1.5 μM), 5-HT dose dependently inhibited adenylate cyclase activity (EC50= 10 ± 2 nM). The inhibitory effect of 5-HT on Ca2+-stimulated adenylate cyclase was antagonized by spiperone (KB= 2 ± 0.8 nM). The rank order of potency of 5-HT agonists to inhibit Ca2+-stimulated adenylate cyclase in the hippocampus was: 5-carboxamidotryptamine (5-CT) > 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) > 5-hydroxytryptamine (5-HT) = 5-methoxytryptamine (5-OCH3-T) > trifluoromethylphenylpiperazine (TFMPP) > m-chlorophenylpiperazine (mCPP). 2-Methyl-5-hydroxytryptamine (2-CH3-5-HT) did not exert an effect on Ca2+-stimulated enzyme activity. In the cerebral cortex 5-HT exerted a biphasic stimulatory effect on adenylate cyclase activity in the absence of Ca2+(EC50= 0.2 ± 0.04 nM and 10 ± 3μM), whereas 8-OH-DPAT, 5-CT and 2-CH3-5-HT exerted a monophasic effect. In the presence of Ca2+(1.5 μM), low cocentrations of 5-HT, 8-OH-DPAT, 5-CT and 2-CH3-5-HT potentiated adenylate cyclase activity, whereas higher concentrations, except 2-CH3-5-HT, inhibited the enzyme activity. We propose that the 5-HT receptor mediating inhibition of Ca2+-stimulated adenylate cyclase in the rat hippocampus corresponds to the 5-HT1Asubtype. 5-HT seems to enhance Ca2+-stimulated adenylate cyclase activity in the cerebral cortex via a non-typical 5-HT receptor, and to reduce enzyme activity via the 5 HT1Areceptor.
使用毛喉素刺激大鼠海马中的腺苷酸环化酶来筛选通过 5-HT1A 受体起作用的化合物。
DOI: --
发表时间: 1988
期刊: Proceedings of the Western Pharmacology Society
影响因子: --
作者:
Cornfield,LJ;Nelson,DL;Monroe,PJ;Taylor,EW;Nikam,SS
通讯作者: Nikam,SS
DOI: 10.1073/pnas.83.11.4086
发表时间: 1986-06-01
影响因子: 11.1
作者:
CONN, PJ;SANDERSBUSH, E;HARTIG, PR
通讯作者: HARTIG, PR
钙调蛋白可能在神经递质介导的大鼠小脑腺苷酸环化酶的抑制和刺激中发挥关键作用。
DOI: --
发表时间: 1987
影响因子: 3.6
作者:
Ahlijanian,MK;Cooper,DM
通讯作者: Cooper,DM
豚鼠和大鼠海马膜中 5-羟色胺 1a 受体介导的毛喉素刺激的腺苷酸环化酶活性抑制作用的表征。
DOI: --
发表时间: 1986
期刊: The Journal of pharmacology and experimental therapeutics
影响因子: --
作者:
DeVivo,M;Maayani,S
通讯作者: Maayani,S
豚鼠海马膜中与腺苷酸环化酶偶联的两种 5-羟色胺受体的药理学特征。
DOI: --
发表时间: 1987
影响因子: 3.6
作者:
Shenker,A;Maayani,S;Weinstein,H;Green,JP
通讯作者: Green,JP