Literature DB >> 1719543

Effect of CP-96,345, a nonpeptide substance P receptor antagonist, on salivation in rats.

R M Snider1, K P Longo, S E Drozda, J A Lowe, S E Leeman.   

Abstract

CP-96,345 [(2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl) methyl]-1-azabicyclo[2.2.2]octan-3-amine) antagonism of substance P-stimulated salivation was investigated in pentobarbital-anesthetized rats. Administered either intraperitoneally or orally, CP-96,345 produced dose-dependent inhibition of the sialogogic response elicited by substance P, with a median effective dose of 12-24 mumol/kg (5-10 mg/kg) of body weight, but had no effect on acetylcholine-stimulated salivation. CP-96,345 produced concentration-dependent inhibition of [3H]substance P binding to rat submaxillary gland membranes, with a median effective concentration of 34 +/- 3.6 nM. These biological activities were confined to CP-96,345 in that the 2R,3R enantiomer (CP-96,344) was without effect.

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Year:  1991        PMID： 1719543      PMCID： PMC52863          DOI： 10.1073/pnas.88.22.10042

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN： 0027-8424            Impact factor:   11.205


  15 in total

1.  The rat submaxillary gland contains predominantly P-type tachykinin binding sites.

Authors:  S H Buck; E Burcher
Journal:  Peptides       Date:  1985 Nov-Dec       Impact factor: 3.750

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Authors:  Y Takeda; J E Krause
Journal:  Proc Natl Acad Sci U S A       Date:  1989-01       Impact factor: 11.205

Review 3.  Tachykinins.

Authors:  J E Maggio
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Review 4.  New selective agonists for neurokinin receptors: pharmacological tools for receptor characterization.

Authors:  D Regoli; G Drapeau; S Dion; R Couture
Journal:  Trends Pharmacol Sci       Date:  1988-08       Impact factor: 14.819

5.  Binding of [3H]substance P to putative substance P receptors in rat brain membranes.

Authors:  M H Perrone; R E Diehl; D R Haubrich
Journal:  Eur J Pharmacol       Date:  1983-11-11       Impact factor: 4.432

6.  Neurokinin-induced salivation in the anesthetized rat: a three receptor hypothesis.

Authors:  C W Murray; A Cowan; D L Wright; J L Vaught; H I Jacoby
Journal:  J Pharmacol Exp Ther       Date:  1987-08       Impact factor: 4.030

7.  Spantide II, an effective tachykinin antagonist having high potency and negligible neurotoxicity.

Authors:  K Folkers; D M Feng; N Asano; R Håkanson; Z Weisenfeld-Hallin; S Leander
Journal:  Proc Natl Acad Sci U S A       Date:  1990-06       Impact factor: 11.205

8.  NK-1 receptors mediate the tachykinin stimulation of salivary secretion: selective agonists provide further evidence.

Authors:  S Giuliani; C A Maggi; D Regoli; G Drapeau; P Rovero; A Meli
Journal:  Eur J Pharmacol       Date:  1988-06-10       Impact factor: 4.432

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Authors:  K Folkers; R Håkanson; J Hörig; J C Xu; S Leander
Journal:  Br J Pharmacol       Date:  1984-10       Impact factor: 8.739

Review 10.  Diversity in mammalian tachykinin peptidergic neurons: multiple peptides, receptors, and regulatory mechanisms.

Authors:  C J Helke; J E Krause; P W Mantyh; R Couture; M J Bannon
Journal:  FASEB J       Date:  1990-04-01       Impact factor: 5.191
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  12 in total

1.  Inhibitory action of (+/-)CP-96,345 on the cardiovascular responses to intrathecal substance P and neuropeptide K in the conscious freely moving rat.

Authors:  T M Pham; R Couture
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-01       Impact factor: 3.000

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Review 3.  Substance P antagonists as a therapeutic approach to improving outcome following traumatic brain injury.

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4.  Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists.

Authors:  J C Beaujouan; E Heuillet; F Petitet; M Saffroy; Y Torrens; J Glowinski
Journal:  Br J Pharmacol       Date:  1993-03       Impact factor: 8.739

5.  Block of voltage-dependent sodium currents by the substance P receptor antagonist (+/-)-CP-96,345 in neurones cultured from rat cortex.

Authors:  M Caeser; G R Seabrook; J A Kemp
Journal:  Br J Pharmacol       Date:  1993-08       Impact factor: 8.739

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Authors:  C Pothoulakis; I Castagliuolo; J T LaMont; A Jaffer; J C O'Keane; R M Snider; S E Leeman
Journal:  Proc Natl Acad Sci U S A       Date:  1994-02-01       Impact factor: 11.205

7.  Use of selective antagonists to dissociate the central cardiovascular and behavioural effects of tachykinins on NK1 and NK2 receptors in the rat.

Authors:  C Tschöpe; P Picard; J Culman; A Prat; K Itoi; D Regoli; T Unger; R Couture
Journal:  Br J Pharmacol       Date:  1992-11       Impact factor: 8.739

8.  Substance P is essential for maintaining gut muscle contractility: a novel role for coneurotransmission revealed by botulinum toxin.

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9.  Enterococcus faecalis overcomes foreign body-mediated inflammation to establish urinary tract infections.

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10.  Involvement of neuronal TGF-β activated kinase 1 in the development of tolerance to morphine-induced antinociception in rat spinal cord.

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