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Histamine in the nervous system.神经系统中的组胺。
Physiol Rev. 2008 Jul;88(3):1183-241. doi: 10.1152/physrev.00043.2007.
2
High-affinity binding of [3H]cimetidine to a heme-containing protein in rat brain.[3H]西咪替丁与大鼠脑中一种含血红素的蛋白质的高亲和力结合。
Drug Metab Dispos. 2008 Mar;36(3):614-21. doi: 10.1124/dmd.107.017889. Epub 2007 Dec 19.
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Histaminergic involvement in neuropathic pain produced by partial ligation of the sciatic nerve in rats.组胺能参与大鼠坐骨神经部分结扎所致的神经性疼痛。
Reg Anesth Pain Med. 2007 Mar-Apr;32(2):124-9. doi: 10.1016/j.rapm.2006.11.009.
4
CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist.CC12是一种用于[3H]西咪替丁结合的高亲和力配体，是一种英普咪定拮抗剂。
Neuropharmacology. 2007 Apr;52(5):1244-55. doi: 10.1016/j.neuropharm.2007.01.004. Epub 2007 Jan 20.
5
Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic.因普罗根化学同系物的抗伤害感受活性：侧链长度的优化导致发现一种新型强效非阿片类镇痛药。
Neuropharmacology. 2006 Sep;51(3):447-56. doi: 10.1016/j.neuropharm.2006.04.003. Epub 2006 Jun 23.
6
Effects of cimetidine-like drugs on recombinant GABAA receptors.西咪替丁类药物对重组GABAA受体的影响。
Life Sci. 2004 Oct 8;75(21):2551-8. doi: 10.1016/j.lfs.2004.05.020.
7
Pain-relieving drugs and the brain histaminergic system: multiple analgesic mechanisms from histamine, improgan and cimetidine.止痛药物与脑组胺能系统：组胺、英普咪定和西咪替丁的多种镇痛机制
Inflamm Res. 2004 Mar;53 Suppl 1:S43-4. doi: 10.1007/s00011-003-0320-7. Epub 2004 Mar 5.
8
Synthetic analgesics. II. Dithienylbutenyl- and dithienylbutylamines.合成镇痛药。II. 二噻吩基丁烯基胺和二噻吩基丁胺。
J Pharmacol Exp Ther. 1953 Mar;107(3):385-93.
9
Improgan antinociception does not require neuronal histamine or histamine receptors.Improgan的抗伤害感受作用并不需要神经元组胺或组胺受体。
Brain Res. 2003 Jun 6;974(1-2):146-52. doi: 10.1016/s0006-8993(03)02572-1.
10
Inhibition of improgan antinociception by the cannabinoid (CB)(1) antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A): lack of obligatory role for endocannabinoids acting at CB(1) receptors.大麻素（CB）1拮抗剂N-（哌啶-1-基）-5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-1H-吡唑-3-甲酰胺（SR141716A）对英普罗根镇痛作用的抑制：内源性大麻素作用于CB1受体并非必要条件
J Pharmacol Exp Ther. 2002 Oct;303(1):314-22. doi: 10.1124/jpet.102.036251.

依普罗君样抗伤害感受性药物对脑 [(3)H]西咪替丁结合的抑制作用。

Inhibition of brain [(3)H]cimetidine binding by improgan-like antinociceptive drugs.

机构信息

Center for Neuropharmacology and Neuroscience, Albany Medical College, NY 12208, USA.

出版信息

Eur J Pharmacol. 2010 Apr 25;632(1-3):33-8. doi: 10.1016/j.ejphar.2010.01.026. Epub 2010 Feb 6.

DOI:10.1016/j.ejphar.2010.01.026
PMID:20138862
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2836490/
Abstract

[(3)H]cimetidine, a radiolabeled histamine H(2) receptor antagonist, binds with high affinity to an unknown hemoprotein in the brain which is not the histamine H(2) receptor. Improgan, a close chemical congener of cimetidine, is a highly effective pain-relieving drug following CNS administration, yet its mechanism of action remains unknown. To test the hypothesis that the [(3)H]cimetidine-binding site is the improgan antinociceptive target, improgan, cimetidine, and 8 other chemical congeners were studied as potential inhibitors of [(3)H]cimetidine binding in membrane fractions from the rat brain. All compounds produced a concentration-dependent inhibition of [(3)H]cimetidine binding over a 500-fold range of potencies (K(i) values were 14.5 to >8000nM). However, antinociceptive potencies in rats did not significantly correlate with [(3)H]cimetidine-binding affinities (r=0.018, p=0.97, n=10). These results suggest that the [(3)H]cimetidine-binding site is not the analgesic target for improgan-like drugs.

摘要

[(3)H]西咪替丁，一种放射性标记的组胺 H（2）受体拮抗剂，与脑中一种未知的血红蛋白高亲和力结合，而不是组胺 H（2）受体。异丙嗪是西咪替丁的紧密化学同系物，在中枢神经系统给药后是一种非常有效的止痛药物，但它的作用机制仍不清楚。为了验证[(3)H]西咪替丁结合位点是异丙嗪镇痛靶点的假设，研究了异丙嗪、西咪替丁和其他 8 种化学同系物作为大鼠脑膜部分[3H]西咪替丁结合的潜在抑制剂。所有化合物在 500 倍的效力范围内产生浓度依赖性抑制[3H]西咪替丁结合（Ki 值为 14.5 至> 8000 nM）。然而，大鼠的镇痛效力与[3H]西咪替丁结合亲和力无显著相关性（r=0.018，p=0.97，n=10）。这些结果表明，[3H]西咪替丁结合位点不是类似异丙嗪药物的镇痛靶点。