• Medientyp: E-Artikel
  • Titel: Tachykinin receptors involved in the contractile effect of the natural tachykinins in the rat gastric fundus
  • Beteiligte: Smits, Geert J. M.; Lefebvre, Remain A.
  • Erschienen: Wiley, 1994
  • Erschienen in: Journal of Autonomic Pharmacology
  • Sprache: Englisch
  • DOI: 10.1111/j.1474-8673.1994.tb00619.x
  • ISSN: 0144-1795; 1365-2680
  • Schlagwörter: Pharmacology ; General Neuroscience
  • Entstehung:
  • Anmerkungen:
  • Beschreibung: <jats:p>1 The receptors involved in mammalian tachykinin‐induced contractions of longitudinal smooth muscle strips of the rat gastric fundus were characterized pharmacologically.</jats:p><jats:p>2 Substance P (SP), neurokinin A, neurokinin B and senktide contracted the strips in a concentration‐dependent manner with a potency order of neurokinin A senktide &gt; neurokinin B &gt; substance P. The contractions were not influenced by tetrodotoxin and atropine.</jats:p><jats:p>3 L 659877, a NK<jats:sub>2B</jats:sub>‐receptor‐preferring antagonist reduced neurokinin A‐ and neurokinin B‐induced contractions (estimated p<jats:italic>K</jats:italic><jats:sub>B</jats:sub> 6.9 and 6.3, respectively) but had less pronounced effects on SP‐induced contractions and none on contractions induced by senktide. MEN 10376, an NK<jats:sub>2A</jats:sub>‐receptor‐preferring antagonist, reduced the neurokinin A‐induced contractions (estimated p<jats:italic>K</jats:italic><jats:sub>a</jats:sub> 5.2), while dactinomycin, reduced the neurokinin A‐induced contractions only to a minor extent at 10<jats:sup>−4</jats:sup> M.</jats:p><jats:p>4 CP 96345, an NK<jats:sub>1</jats:sub>‐receptor antagonist, reduced substance P‐ and neurokinin A‐induced responses, but also reduced the contractions induced by KC1 and methacholine. RP 67580, another non‐peptide NK<jats:sub>1</jats:sub>‐receptor antagonist had no effect on the substance P‐, neurokinin A‐ and neurokinin B‐induced contractions up to a concentration of 3 × 10<jats:sup>−6</jats:sup> M.</jats:p><jats:p>5 These results suggest that the mammalian tachykinins induce contractions of the longitudinal smooth muscle strip of the rat gastric fundus by direct action at muscular NK<jats:sub>2B</jats:sub>‐ and NK<jats:sub>3</jats:sub>‐receptors.</jats:p>