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1
(+/-)-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.
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
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4
Comparison of spantide II and CP-96,345 for blockade of tachykinin-evoked contractions of smooth muscle.用于阻断速激肽诱发的平滑肌收缩的spantide II和CP-96,345的比较。
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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。
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Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345.使用非肽拮抗剂CP-96,345对速激肽NK1受体中的物种变体进行研究。
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Am J Physiol Gastrointest Liver Physiol. 2014 May 15;306(10):G839-48. doi: 10.1152/ajpgi.00436.2012. Epub 2014 Apr 3.
2
Tachykinins stimulate release of peptide hormones (glucagon-like peptide-1) and paracrine (somatostatin) and neurotransmitter (vasoactive intestinal polypeptide) from porcine ileum through NK-1 receptors.速激肽通过NK-1受体刺激猪回肠释放肽类激素（胰高血糖素样肽-1）、旁分泌物质（生长抑素）和神经递质（血管活性肠肽）。
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Substance P contributes to rapidly adapting receptor responses to pulmonary venous congestion in rabbits.P物质有助于家兔对肺静脉充血的快速适应性受体反应。
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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。
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6
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。
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7
Presence of neuropeptide Y in the rat seminal vesicle and its effects on noradrenaline- and nerve-induced contractions.大鼠精囊内神经肽Y的存在及其对去甲肾上腺素和神经诱导收缩的影响。
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8
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。
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Effects of the tachykinin NK1 receptor antagonist, RP 67580, on central cardiovascular and behavioural effects of substance P, neurokinin A and neurokinin B.速激肽NK1受体拮抗剂RP 67580对P物质、神经激肽A和神经激肽B的中枢心血管及行为效应的影响
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10
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本文引用的文献

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Immunohistochemical localization of substance P, vasoactive intestinal polypeptide and gastrin-releasing peptide in vas deferens and seminal vesicle, and the effect of these and eight other neuropeptides on resting tension and neurally evoked contractile activity.P物质、血管活性肠肽和胃泌素释放肽在输精管和精囊中的免疫组织化学定位，以及这些和其他八种神经肽对静息张力和神经诱发收缩活动的影响。
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A specific substance P antagonist blocks smooth muscle contractions induced by non-cholinergic, non-adrenergic nerve stimulation.一种特异性P物质拮抗剂可阻断由非胆碱能、非肾上腺素能神经刺激所引起的平滑肌收缩。
Nature. 1981 Dec 3;294(5840):467-9. doi: 10.1038/294467a0.
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Neurogenic mechanisms in control of the rabbit iris sphincter muscle.
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Tachykinins.速激肽
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New selective agonists for neurokinin receptors: pharmacological tools for receptor characterization.神经激肽受体的新型选择性激动剂：用于受体表征的药理学工具。
Trends Pharmacol Sci. 1988 Aug;9(8):290-5. doi: 10.1016/0165-6147(88)90013-2.
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Novel substance P antagonist, CP-96,345, blocks responses of cat spinal dorsal horn neurons to noxious cutaneous stimulation and to substance P.新型P物质拮抗剂CP-96,345可阻断猫脊髓背角神经元对有害皮肤刺激和P物质的反应。
Neurosci Lett. 1991 Oct 28;132(1):39-43. doi: 10.1016/0304-3940(91)90428-v.
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Role of NK1 tachykinin receptors in thermonociception: effect of (+/-)-CP 96,345, a non-peptide substance P antagonist, on the hot plate test in mice.
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Receptor-selective, peptidase-resistant agonists at neurokinin NK-1 and NK-2 receptors: new tools for investigating neurokinin function.
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（±）-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。

(+/-)-CP-96,345, a selective tachykinin NK1 receptor antagonist, has non-specific actions on neurotransmission.

作者信息

Wang Z Y, Håkanson R

机构信息

Department of Pharmacology, University of Lund, Sweden.

出版信息

Br J Pharmacol. 1992 Nov;107(3):762-5. doi: 10.1111/j.1476-5381.1992.tb14520.x.

DOI:10.1111/j.1476-5381.1992.tb14520.x
PMID:1335338
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1907737/
Abstract
  1. The non-specific effects of the non-peptide tachykinin receptor antagonist (+/-)-CP-96,345, were assessed in several smooth muscle-nerve preparations. The preparations were the iris sphincter muscle of the rabbit and the taenia coli, vas deferens and seminal vesicle of the guinea-pig. 2. (+/-)-CP-96,345 concentration-dependently inhibited the electrically evoked, tachykinin-mediated contractile responses of the iris sphincter and the taenia coli. The pIC50 values were 5.4 +/- 0.2 (mean +/- s.e.mean) and 5.7 +/- 0.08 respectively. 3. (+/-)-CP-96,345 also inhibited non-tachykinin-mediated contractile responses to electrical stimulation of the iris sphincter, taenia coli, vas deferens and seminal vesicle. The pIC50 values were 4.3 +/- 0.02, 4.8 +/- 0.03, 4.7 +/- 0.02 and 4.4 +/- 0.05 respectively. These values differ significantly from the pIC50 values of the inhibition of the tachykinin-mediated response in the iris sphincter and taenia coli. 4. (+/-)-CP-96,345 was without effect on carbachol- and noradrenaline-evoked contractions of the iris sphincter but inhibited carbachol- and prostaglandin F2 alpha (PGF2 alpha)-evoked contractions of the taenia coli. 5. We suggest that (+/-)-CP-96,345, apart from its NK1 receptor blocking activity, induces non-specific suppression of neurotransmission, exerted at both pre- and post-junctional sites.
摘要
  1. 在几种平滑肌-神经标本中评估了非肽速激肽受体拮抗剂（±）-CP-96,345的非特异性作用。这些标本包括兔虹膜括约肌以及豚鼠的结肠带、输精管和精囊。2. （±）-CP-96,345浓度依赖性地抑制了虹膜括约肌和结肠带由电刺激诱发的、速激肽介导的收缩反应。其半数抑制浓度的负对数（pIC50）值分别为5.4±0.2（平均值±标准误均值）和5.7±0.08。3. （±）-CP-96,345还抑制了虹膜括约肌、结肠带、输精管和精囊对电刺激的非速激肽介导的收缩反应。其pIC50值分别为4.3±0.02、4.8±0.03、4.7±0.02和4.4±0.05。这些值与抑制虹膜括约肌和结肠带中速激肽介导反应的pIC50值有显著差异。4. （±）-CP-96,345对卡巴胆碱和去甲肾上腺素诱发的虹膜括约肌收缩无影响，但抑制了卡巴胆碱和前列腺素F2α（PGF2α）诱发的结肠带收缩。5. 我们认为，（±）-CP-96,345除了具有NK1受体阻断活性外，还能在神经节前和节后位点非特异性地抑制神经传递。