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A novel, selective radioligand, [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), for the tachykinin NK-2 receptor.

作者信息

Badgery-Parker T, Zeng X P, Lavielle S, Burcher E

机构信息

School of Physiology and Pharmacology, University of New South Wales, Sydney, Australia.

出版信息

Regul Pept. 1993 Jul 2;46(1-2):455-7. doi: 10.1016/0167-0115(93)90118-r.

DOI:10.1016/0167-0115(93)90118-r
PMID:8210504
Abstract

A new radioligand, [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), based on the selective agonist [Lys5,MeLeu9,Nle10]-NKA(4-10) has been developed. Binding in rat fundus membranes was displaced by NP gamma > NKA > or = [Lys5,MeLeu9,Nle10]-NK(4-10) > neuropeptide K > [Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10) > SP > [Sar9,Met(O2)11]-SP >> senktide, indicating binding to NK-2 receptors. Preliminary studies demonstrated high specific binding in membranes from rat urinary bladder, duodenum and colon. Specific binding in rat brain and lung was negligible, and binding in a range of guinea-pig tissues was no more than 35% specific. These data may indicate species differences in NK-2 receptors.

摘要

相似文献

1
A novel, selective radioligand, [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10), for the tachykinin NK-2 receptor.
Regul Pept. 1993 Jul 2;46(1-2):455-7. doi: 10.1016/0167-0115(93)90118-r.
2
Characterisation of a novel, selective radioligand, [125I][Lys5,Tyr(I2)7,MeLeu9,Nle10]neurokinin A-(4-10), for the tachykinin NK2 receptor in rat fundus.新型选择性放射性配体[125I][赖氨酸5,酪氨酸(碘2)7,甲基亮氨酸9,正亮氨酸10]神经激肽A-(4-10)对大鼠胃底速激肽NK2受体的表征
Eur J Pharmacol. 1993 Mar 23;233(2-3):201-7. doi: 10.1016/0014-2999(93)90051-i.
3
Evidence for tachykinin NK-2 receptors in guinea-pig airways from binding and functional studies, using [125I]-[Lys5,Tyr(I2)7,MeLeu9,Nle10]-NKA(4-10).使用[125I]-[赖氨酸5,酪氨酸(碘代2)7,甲基亮氨酸9,正亮氨酸10]-神经激肽A(4-10),通过结合和功能研究获得豚鼠气道中速激肽NK-2受体的证据。
Neuropeptides. 1994 Jan;26(1):1-9. doi: 10.1016/0143-4179(94)90086-8.
4
Binding and functional potency of neurokinin A analogues in the rat fundus: A structure-activity study.神经激肽A类似物在大鼠胃底的结合及功能效价:一项构效关系研究。
Pharmacology. 1999 May;58(5):227-35. doi: 10.1159/000028285.
5
Radioligand binding, autoradiographic and functional studies demonstrate tachykinin NK-2 receptors in dog urinary bladder.
J Pharmacol Exp Ther. 1996 Oct;279(1):423-34. doi: 10.1163/2211730x96x00225.
6
Characterization of tachykinin NK2 receptors in human urinary bladder.人膀胱中速激肽NK2受体的特性研究
J Urol. 1995 May;153(5):1688-92.
7
Autoradiographic localization of tachykinin NK2 and NK1 receptors in the guinea-pig lung, using selective radioligands.使用选择性放射性配体对豚鼠肺中速激肽NK2和NK1受体进行放射自显影定位。
Eur J Pharmacol. 1996 Sep 12;311(2-3):177-86. doi: 10.1016/0014-2999(96)00412-8.
8
Characterization and autoradiographic localization of tachykinin receptors in rat gastric fundus.大鼠胃底速激肽受体的表征及放射自显影定位
J Pharmacol Exp Ther. 1993 Aug;266(2):1043-53.
9
Binding sites for [125I]-Bolton-Hunter scyliorhinin II in guinea-pig ileum: a radioligand binding, functional and autoradiographic study.豚鼠回肠中[125I]-博尔顿-亨特氏鲨肌肽II的结合位点:一项放射性配体结合、功能及放射自显影研究
Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):301-9. doi: 10.1007/BF00175036.
10
Characterization of the [125I]-neurokinin A binding site in the circular muscle of human colon.人结肠环行肌中[125I] - 神经激肽A结合位点的特性研究
Br J Pharmacol. 1999 Jul;127(5):1105-10. doi: 10.1038/sj.bjp.0702648.

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