FK 888作为速激肽NK1受体拮抗剂的特异性研究。
Investigation of the specificity of FK 888 as a tachykinin NK1 receptor antagonist.
作者信息
Wang Z Y, Tung S R, Strichartz G R, Håkanson R
机构信息
Department of Pharmacology, University of Lund, Sweden.
出版信息
Br J Pharmacol. 1994 Apr;111(4):1342-6. doi: 10.1111/j.1476-5381.1994.tb14892.x.
Abstract
- A recently described peptide tachykinin (NK1) receptor antagonist, FK 888, was found to inhibit the electrically-evoked, tachykinin-mediated contractile responses of the rabbit iris sphincter in a concentration-dependent manner; the pIC50 value was 6.6 +/- 0.08. 2. Contractions induced by a selective NK1 receptor agonist, [Sar9,Met(O2)11]substance P, were inhibited competitively by FK 888; the pKB value was 7.1. 3. FK 888 (1 nM-100 microM) was without effect on the electrically-evoked, cholinergic response of the rabbit iris sphincter and the electrically-evoked, sympathetic response of the guinea-pig vas deferens. The contractions of the rabbit iris sphincter, induced by either carbachol (10 nM-30 microM) or noradrenaline (0.1-100 microM), were not affected by 10 microM FK 888. 4. FK 888 (1-30 microM) did not induce histamine release from rat peritoneal mast cells. 5. FK 888 (33 and 333 microM) was without effect on the electrically-evoked action potentials of the frog sciatic nerve. Thus, FK 888 is a moderately high affinity and selective tachykinin (NK1) receptor antagonist.
摘要
- 最近描述的一种肽速激肽（NK1）受体拮抗剂FK 888，被发现能以浓度依赖的方式抑制兔虹膜括约肌由电诱发的、速激肽介导的收缩反应；pIC50值为6.6±0.08。2. 选择性NK1受体激动剂[Sar9,Met(O2)11]P物质诱导的收缩，被FK 888竞争性抑制；pKB值为7.1。3. FK 888（1 nM - 100 μM）对兔虹膜括约肌的电诱发胆碱能反应以及豚鼠输精管的电诱发交感反应均无影响。由卡巴胆碱（10 nM - 30 μM）或去甲肾上腺素（0.1 - 100 μM）诱导的兔虹膜括约肌收缩，不受10 μM FK 888的影响。4. FK 888（1 - 30 μM）不会诱导大鼠腹膜肥大细胞释放组胺。5. FK 888（33和333 μM）对蛙坐骨神经的电诱发动作电位无影响。因此，FK 888是一种具有中等高亲和力的选择性速激肽（NK1）受体拮抗剂。
相似文献
1
Investigation of the specificity of FK 888 as a tachykinin NK1 receptor antagonist.FK 888作为速激肽NK1受体拮抗剂的特异性研究。
Br J Pharmacol. 1994 Apr;111(4):1342-6. doi: 10.1111/j.1476-5381.1994.tb14892.x.
2
Non-specific actions of the non-peptide tachykinin receptor antagonists, CP-96,345, RP 67580 and SR 48968, on neurotransmission.非肽类速激肽受体拮抗剂CP-96,345、RP 67580和SR 48968对神经传递的非特异性作用。
Br J Pharmacol. 1994 Jan;111(1):179-84. doi: 10.1111/j.1476-5381.1994.tb14041.x.
3
Pharmacological assessment of spantide II analogues.斯潘替德II类似物的药理学评估。
Eur J Pharmacol. 1994 Aug 1;260(2-3):121-8. doi: 10.1016/0014-2999(94)90327-1.
4
Tachykinin NK1 and NK2 receptor antagonists and atropine-resistant ascending excitatory reflex to the circular muscle of the guinea-pig ileum.速激肽NK1和NK2受体拮抗剂与豚鼠回肠环形肌的阿托品抵抗性上行兴奋性反射
Br J Pharmacol. 1994 May;112(1):161-8. doi: 10.1111/j.1476-5381.1994.tb13046.x.
5
(+/-)-CP-96,345, a selective tachykinin NK1 receptor antagonist, has non-specific actions on neurotransmission.（±）-CP-96,345，一种选择性速激肽NK1受体拮抗剂，对神经传递有非特异性作用。
Br J Pharmacol. 1992 Nov;107(3):762-5. doi: 10.1111/j.1476-5381.1992.tb14520.x.
6
In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists.利用选择性非肽类NK3受体拮抗剂对兔眼中NK3受体进行体外和体内表征。
Br J Pharmacol. 1997 Oct;122(3):469-76. doi: 10.1038/sj.bjp.0701406.
7
Comparison of tachykinin NK1 and NK2 receptors in the circular muscle of the guinea-pig ileum and proximal colon.豚鼠回肠和近端结肠环形肌中速激肽NK1和NK2受体的比较。
Br J Pharmacol. 1994 May;112(1):150-60. doi: 10.1111/j.1476-5381.1994.tb13045.x.
8
Characterization of NK3 receptors in rabbit isolated iris sphincter muscle.兔离体虹膜括约肌中NK3受体的特性研究
Br J Pharmacol. 1997 Jan;120(1):93-101. doi: 10.1038/sj.bjp.0700867.
9
Evidence that tachykinin NK1 and NK2 receptors mediate non-adrenergic non-cholinergic excitation and contraction in the circular muscle of guinea-pig duodenum.速激肽NK1和NK2受体介导豚鼠十二指肠环行肌非肾上腺素能非胆碱能兴奋和收缩的证据。
Br J Pharmacol. 1995 May;115(2):237-46. doi: 10.1111/j.1476-5381.1995.tb15869.x.
10
Evidence that tachykinins relax the guinea-pig trachea via nitric oxide release and by stimulation of a septide-insensitive NK1 receptor.速激肽通过释放一氧化氮和刺激对七肽不敏感的NK1受体使豚鼠气管舒张的证据。
Br J Pharmacol. 1996 Mar;117(6):1270-6. doi: 10.1111/j.1476-5381.1996.tb16725.x.
引用本文的文献
1
A Multi-Omics Network of a Seven-Gene Prognostic Signature for Non-Small Cell Lung Cancer.一个包含七个基因预后标志物的非小细胞肺癌多组学网络。
Int J Mol Sci. 2021 Dec 25;23(1):219. doi: 10.3390/ijms23010219.
2
Neurogenic inflammation in lung disease: burnt out?肺部疾病中的神经源性炎症：熄灭了？
Inflammopharmacology. 1997;5(4):319-29. doi: 10.1007/s10787-997-0029-2.
3
Stress inhibits hair growth in mice by induction of premature catagen development and deleterious perifollicular inflammatory events via neuropeptide substance P-dependent pathways.应激通过神经肽P物质依赖性途径诱导小鼠毛囊过早进入退行期并引发有害的毛囊周围炎症反应，从而抑制毛发生长。
Am J Pathol. 2003 Mar;162(3):803-14. doi: 10.1016/S0002-9440(10)63877-1.
4
Characterization of tachykinin receptors mediating plasma extravasation and vasodilatation in normal and acutely inflamed knee joints of the rat.介导大鼠正常和急性炎症膝关节血浆外渗及血管舒张的速激肽受体的特性研究
Br J Pharmacol. 1996 Aug;118(8):2107-14. doi: 10.1111/j.1476-5381.1996.tb15650.x.
5
The tachykinin NK1 receptor mediates the migration-promoting effect of substance P on human skin fibroblasts in culture.速激肽NK1受体介导了P物质对培养的人皮肤成纤维细胞的促迁移作用。
Naunyn Schmiedebergs Arch Pharmacol. 1996 Apr;353(5):475-81. doi: 10.1007/BF00169165.
6
'Sensory-efferent' neural control of mucus secretion: characterization using tachykinin receptor antagonists in ferret trachea in vitro.黏液分泌的“感觉-传出”神经控制：在雪貂气管体外实验中使用速激肽受体拮抗剂进行的特征研究
Br J Pharmacol. 1994 Dec;113(4):1183-90. doi: 10.1111/j.1476-5381.1994.tb17122.x.
本文引用的文献
1
Block of voltage-dependent sodium currents by the substance P receptor antagonist (+/-)-CP-96,345 in neurones cultured from rat cortex.P物质受体拮抗剂（±）-CP-96,345对大鼠皮层培养神经元中电压依赖性钠电流的阻断作用
Br J Pharmacol. 1993 Aug;109(4):918-24. doi: 10.1111/j.1476-5381.1993.tb13708.x.
2
Tachykinin receptors mediating responses to sensory nerve stimulation and exogenous tachykinins and analogues in the rabbit isolated iris sphincter.速激肽受体介导兔离体虹膜括约肌对感觉神经刺激及外源性速激肽和类似物的反应。
Br J Pharmacol. 1993 Aug;109(4):1008-13. doi: 10.1111/j.1476-5381.1993.tb13721.x.
3
Tachykinin receptors and tachykinin receptor antagonists.速激肽受体与速激肽受体拮抗剂
J Auton Pharmacol. 1993 Feb;13(1):23-93. doi: 10.1111/j.1474-8673.1993.tb00396.x.
4
Receptor subtypes or species homologues: relevance to drug discovery.受体亚型或物种同源物：与药物发现的相关性。
Trends Pharmacol Sci. 1993 Oct;14(10):376-83. doi: 10.1016/0165-6147(93)90096-3.
5
Non-specific actions of the non-peptide tachykinin receptor antagonists, CP-96,345, RP 67580 and SR 48968, on neurotransmission.非肽类速激肽受体拮抗剂CP-96,345、RP 67580和SR 48968对神经传递的非特异性作用。
Br J Pharmacol. 1994 Jan;111(1):179-84. doi: 10.1111/j.1476-5381.1994.tb14041.x.
6
The interaction of the NK1 receptor antagonist CP-96,345 with L-type calcium channels and its functional consequences.NK1受体拮抗剂CP-96,345与L型钙通道的相互作用及其功能后果。
Br J Pharmacol. 1993 Sep;110(1):385-91. doi: 10.1111/j.1476-5381.1993.tb13821.x.
7
Does substance P release mediate NANC nerve-mediated responses to field stimulation and ligands, in the rabbit isolated sphincter pupillae?在兔离体瞳孔括约肌中，P物质释放是否介导了非肾上腺素能非胆碱能（NANC）神经介导的对场刺激和配体的反应？
Regul Pept. 1993 Jul 2;46(1-2):278-81. doi: 10.1016/0167-0115(93)90059-h.
8
The rabbit iris sphincter contains NK1 and NK3 but not NK2 receptors: a study with selective agonists and antagonists.兔虹膜括约肌含有NK1和NK3受体，但不含NK2受体：一项使用选择性激动剂和拮抗剂的研究。
Regul Pept. 1993 Apr 8;44(3):269-75. doi: 10.1016/0167-0115(93)90136-v.
9
Neurotransmitter functions of mammalian tachykinins.哺乳动物速激肽的神经递质功能。
Physiol Rev. 1993 Apr;73(2):229-308. doi: 10.1152/physrev.1993.73.2.229.
10
Analysis of a nonpeptide antagonist for substance P on myenteric neurons of guinea-pig small intestine.P物质非肽拮抗剂对豚鼠小肠肌间神经元的作用分析
Eur J Pharmacol. 1993 Mar 2;232(2-3):235-9. doi: 10.1016/0014-2999(93)90779-h.
Zotero 插件