Literature DB >> 7830490

SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor.

X Emonds-Alt1, D Bichon, J P Ducoux, M Heaulme, B Miloux, M Poncelet, V Proietto, D Van Broeck, P Vilain, G Neliat.   

Abstract

SR 142801 is the first potent and selective non-peptide antagonist of the tachykinin NK3 receptor. It inhibited [MePhe7]NKB binding to its receptor from various species, including humans. SR 142801 was a competitive antagonist of [MePhe7]NKB-mediated contractions of guinea-pig ileum and inhibited the acetylcholine release following the activation of the guinea-pig ileum tachykinin NK3 receptor. In vivo, SR 142801 potently inhibited the turning behaviour induced by intrastriatal injection of senktide in gerbils, and appears as a powerful tool for investigation of the physiological and pathological role of NKB and its NK3 receptor.

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Year:  1995        PMID： 7830490     DOI： 10.1016/0024-3205(94)00413-m

Source DB:  PubMed          Journal:  Life Sci        ISSN： 0024-3205            Impact factor:   5.037


  33 in total

1.  Respiratory actions of tachykinins in the nucleus of the solitary tract: characterization of receptors using selective agonists and antagonists.

Authors:  S B Mazzone; D P Geraghty
Journal:  Br J Pharmacol       Date:  2000-03       Impact factor: 8.739

2.  Tachykinin-induced contraction of the guinea-pig isolated oesophageal mucosa is mediated by NK(2) receptors.

Authors:  K P Kerr; B Thai; I M Coupar
Journal:  Br J Pharmacol       Date:  2000-12       Impact factor: 8.739

3.  Functional characterization of tachykinin NK1 receptors in the mouse uterus.

Authors:  Eva Patak; Jocelyn N Pennefather; Anna Fleming; Margot E Story
Journal:  Br J Pharmacol       Date:  2002-12       Impact factor: 8.739

Review 4.  Neuropeptide receptor ligands as drugs for psychiatric diseases: the end of the beginning?

Authors:  Guy Griebel; Florian Holsboer
Journal:  Nat Rev Drug Discov       Date:  2012-05-18       Impact factor: 84.694

5.  Characterization of RO4583298 as a novel potent, dual antagonist with in vivo activity at tachykinin NK₁ and NK₃ receptors.

Authors:  P Malherbe; F Knoflach; M C Hernandez; T Hoffmann; P Schnider; R H Porter; J G Wettstein; T M Ballard; W Spooren; L Steward
Journal:  Br J Pharmacol       Date:  2011-02       Impact factor: 8.739

6.  Regional variations in neurokinin receptor subtype contributions to muscularis mucosae and epithelial function in rat colon.

Authors:  Caroline B Appleyard; Marangelie Morales; William H Percy
Journal:  Dig Dis Sci       Date:  2006-03       Impact factor: 3.199

7.  Differential role of tachykinin NK3 receptors on cholinergic excitatory neurotransmission in the mouse stomach and small intestine.

Authors:  J G De Man; B Y De Winter; H U De Schepper; A G Herman; P A Pelckmans
Journal:  Br J Pharmacol       Date:  2008-09-22       Impact factor: 8.739

8.  Effect of the tachykinin receptor antagonists, SR 140333, FK 888, and SR 142801, on capsaicin-induced mouse ear oedema.

Authors:  H Inoue; N Nagata; Y Koshihara
Journal:  Inflamm Res       Date:  1996-06       Impact factor: 4.575

9.  Study of SR 142801, a new potent non-peptide NK3 receptor antagonist on cardiovascular responses in conscious guinea-pig.

Authors:  A Roccon; D Marchionni; D Nisato
Journal:  Br J Pharmacol       Date:  1996-07       Impact factor: 8.739

10.  Involvement of tachykinin receptors in oedema formation and plasma extravasation induced by substance P, neurokinin A, and neurokinin B in mouse ear.

Authors:  H Inoue; N Nagata; Y Koshihara
Journal:  Inflamm Res       Date:  1996-07       Impact factor: 4.575
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