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。
Investigation into species variants in tachykinin NK1 receptors by use of the non-peptide antagonist, CP-96,345.
作者信息
Beresford I J, Birch P J, Hagan R M, Ireland S J
机构信息
Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Hertfordshire.
出版信息
Br J Pharmacol. 1991 Oct;104(2):292-3. doi: 10.1111/j.1476-5381.1991.tb12423.x.
Abstract
The affinity of the non-peptide antagonist CP-96,345 for tachykinin NK1 receptors has been estimated in a range of species by use of both radioligand binding and functional assays. CP-96,345 was 30-120 fold less active at NK1 receptors in rat and mouse than in the other species examined, including man. These results demonstrate the existence of species variations in NK1 receptors.
摘要
通过放射性配体结合和功能测定，已在一系列物种中估计了非肽拮抗剂CP - 96,345对速激肽NK1受体的亲和力。与包括人类在内的其他受试物种相比，CP - 96,345在大鼠和小鼠的NK1受体上的活性要低30至120倍。这些结果证明了NK1受体存在物种差异。
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本文引用的文献
1
Receptors for substance P. I. The pharmacological preparations.
Eur J Pharmacol. 1984 Jan 27;97(3-4):161-70. doi: 10.1016/0014-2999(84)90447-3.
2
Pharmacological characterization and autoradiographic localization of substance P receptors in guinea pig brain.豚鼠脑内P物质受体的药理学特性及放射自显影定位
Peptides. 1986 Sep-Oct;7(5):855-64. doi: 10.1016/0196-9781(86)90106-3.
3
Mammalian tachykinin receptors.哺乳动物速激肽受体
Annu Rev Neurosci. 1991;14:123-36. doi: 10.1146/annurev.ne.14.030191.001011.
4
Species differences in affinities of non-peptide antagonists for substance P receptors.
Eur J Pharmacol. 1991 May 17;197(2-3):237-8. doi: 10.1016/0014-2999(91)90532-u.
5
A potent nonpeptide antagonist of the substance P (NK1) receptor.一种有效的P物质（NK1）受体非肽拮抗剂。
Science. 1991 Jan 25;251(4992):435-7. doi: 10.1126/science.1703323.
6
Receptors mediating tachykinin-induced contractile responses in guinea-pig trachea.介导豚鼠气管速激肽诱导收缩反应的受体。
Br J Pharmacol. 1991 Jun;103(2):1463-9. doi: 10.1111/j.1476-5381.1991.tb09812.x.
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