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拟抗精神病药去酪氨酸1-γ-内啡肽对体内3H-螺哌隆结合的抑制作用。

Inhibition of in vivo 3H-spiperone binding by the proposed antipsychotic Des-Tyr1-gamma-endorphin.

作者信息

Pedigo N W, Schallert T, Overstreet D H, Ling N C, Ragan P, Reisine T D, Yamamura H I

出版信息

Eur J Pharmacol. 1979 Dec 20;60(4):359-64. doi: 10.1016/0014-2999(79)90242-5.

DOI:10.1016/0014-2999(79)90242-5
PMID:43261
Abstract

The proposed antipsychotic neuropeptide des-tyrosine1-gamma-endorphin (DT gamma E, beta LPH62,77) inhibits in vivo 3H-spiperone binding in the hypothalamus, corpus striatum and mesolimbic areas of rat brain. The neuroleptic drug haloperidol produces similar effects in these areas as well as in frontal cortex, but is considerably more potent than DT gamma E. Correspondingly, haloperidol produces postural and motor abnormalities not seen with DY gamma E. These data together with the results from previous in vitro studies suggest DT gamma E might act indirectly, having a selective neuroleptic-like action at 3H-spiperone binding sites.

摘要

所提出的抗精神病神经肽去酪氨酸1-γ-内啡肽(DTγE,β-LPH62,77)可抑制大鼠脑下丘脑、纹状体和中脑边缘区的体内3H-螺哌隆结合。抗精神病药物氟哌啶醇在这些区域以及额叶皮质也产生类似作用,但比DTγE的效力强得多。相应地,氟哌啶醇会产生DTγE未出现的姿势和运动异常。这些数据以及先前体外研究的结果表明,DTγE可能间接起作用,在3H-螺哌隆结合位点具有选择性的类抗精神病作用。

相似文献

1
Inhibition of in vivo 3H-spiperone binding by the proposed antipsychotic Des-Tyr1-gamma-endorphin.拟抗精神病药去酪氨酸1-γ-内啡肽对体内3H-螺哌隆结合的抑制作用。
Eur J Pharmacol. 1979 Dec 20;60(4):359-64. doi: 10.1016/0014-2999(79)90242-5.
2
Lack of effect of des-tyrosine1-gamma-endorphin on in vivo [3H]spiperone binding.
Eur J Pharmacol. 1982 May 7;80(1):127-9. doi: 10.1016/0014-2999(82)90187-x.
3
In vivo interaction of gamma-type endorphins with dopaminergic ligands in rat brain.大鼠脑内γ型内啡肽与多巴胺能配体的体内相互作用。
Eur J Pharmacol. 1983 Apr 8;88(4):365-70. doi: 10.1016/0014-2999(83)90587-3.
4
Neuroleptic activity of the neuropeptide beta-LPH62-77 ([Des-Tyr1]gamma-endorphin; DT gamma E).神经肽β-促脂解素62-77([去酪氨酸1]γ-内啡肽;DTγE)的抗精神病活性。
Eur J Pharmacol. 1978 Jun 15;49(4):427-36. doi: 10.1016/0014-2999(78)90317-5.
5
Examination of des-tyrosine1-gamma-endorphin activity at oH-spiroperidol binding sites in rat brain.
Life Sci. 1979 Apr 30;24(18):1645-9. doi: 10.1016/0024-3205(79)90247-9.
6
Electroencephalographic changes in the lateral septum complex following systemic administration of des-Tyr1 -alpha-endorphin, des-Tyr1-gamma-endorphin and haloperidol in rats.大鼠全身注射去酪氨酸1-α-内啡肽、去酪氨酸1-γ-内啡肽和氟哌啶醇后外侧隔复合体的脑电图变化
Life Sci. 1982 Nov 29;31(22):2417-24. doi: 10.1016/0024-3205(82)90745-7.
7
[Des-1-tyrosine-gamma-endorphin: an assessment of its neuroleptic properties and effect on dopamine synthesis].[去-1-酪氨酸-γ-内啡肽:对其抗精神病特性及对多巴胺合成影响的评估]
Farmakol Toksikol. 1982 Sep-Oct;45(5):5-8.
8
Effect of morphine, beta-endorphin and leu-enkephalin on 3H-spiroperidol binding to bovine pituitary membranes.
Life Sci. 1979 Aug 6;25(6):531-5. doi: 10.1016/0024-3205(79)90566-6.
9
Effects of chronic haloperidol, thioridazine and zotepine treatment on apomorphine elicited stereotypic behavior and 3H-spiroperidol binding sites in the striatum of the rat.慢性氟哌啶醇、硫利达嗪和佐替平治疗对阿扑吗啡诱发的大鼠纹状体刻板行为及3H-螺哌啶醇结合位点的影响。
Proc West Pharmacol Soc. 1981;24:5-6.
10
Possible role of opiate receptors and des-tyrosine1-gamma-endorphin in schizophrenia.
Adv Biochem Psychopharmacol. 1980;22:549-62.

引用本文的文献

1
Modification of the behavioural effects of haloperidol and of dopamine receptor regulation by altered thyroid status.甲状腺状态改变对氟哌啶醇行为效应及多巴胺受体调节的影响
Psychopharmacology (Berl). 1984;82(1-2):102-6. doi: 10.1007/BF00426390.
2
Further characterization of opioid receptors in the striatum mediating muscular rigidity in rats.介导大鼠肌肉强直的纹状体中阿片受体的进一步特征研究。
Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):321-5. doi: 10.1007/BF00501313.
3
Calcium alters the sensitivity of intact horizontal cells to dopamine antagonists.
钙会改变完整水平细胞对多巴胺拮抗剂的敏感性。
Proc Natl Acad Sci U S A. 1982 May;79(10):3350-4. doi: 10.1073/pnas.79.10.3350.
4
Effect of des-Tyr1-gamma-endorphin on serotonin metabolism in rat brain regions.
Experientia. 1982 May 15;38(5):598-9. doi: 10.1007/BF02327070.