Pharmacological characterization of tachykinin-stimulated inositol phospholipid hydrolysis in peripheral tissues

Br J Pharmacol. 1990 Dec;101(4):1001-5. doi: 10.1111/j.1476-5381.1990.tb14196.x.

Abstract

1. Tachykinin-stimulated inositol phospholipid hydrolysis was examined in slices of rat parotid gland, hamster urinary bladder and guinea-pig ileum longitudinal muscle. 2. In the presence of lithium, substance P and other naturally-occurring and synthetic tachykinins induced large, dose-dependent increases in [3H]-inositol monophosphate accumulation. 3. In slices of rat parotid gland, [pGlu6,L-Pro9]SP(6-11) was considerably more potent in stimulating inositol phospholipid hydrolysis than [pGlu6,D-Pro9]SP(6-11). 4. In contrast, in slices of hamster urinary bladder, [pGlu6,D-Pro9]SP(6-11) exhibited greater potency in evoking inositol phospholipid breakdown than [pGlu6,L-Pro9]SP(6-11). 5. The differential selectivity of these C-terminal fragments of substance P suggests that they may be useful tools for distinguishing between NK1 and NK2 receptors. 6. L-659,837 and L-659,874 antagonized eledoisin-stimulated inositol phospholipid hydrolysis in slices of hamster urinary bladder. Neither compound significantly reduced substance-P evoked inositol phospholipid breakdown in slices of rat parotid gland, or senktide-induced inositol phospholipid hydrolysis in slices of guinea-pig ileum. 7. L-659,837 and L-659,874 had no effect on the atropine-sensitive, carbachol-stimulated inositol phospholipid hydrolysis in slices of rat parotid gland. 8. These data further support the notion that L-659,837 and L-659,874 are potent and selective NK2 receptor antagonists.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Cricetinae
  • Guinea Pigs
  • Hydrolysis
  • Ileum / drug effects
  • Ileum / metabolism
  • In Vitro Techniques
  • Muscles / drug effects
  • Muscles / metabolism
  • Parotid Gland / drug effects
  • Parotid Gland / metabolism
  • Peptide Fragments / pharmacology
  • Peptides, Cyclic / pharmacology
  • Phosphatidylinositols / metabolism*
  • Pyrrolidonecarboxylic Acid / analogs & derivatives
  • Rats
  • Substance P / analogs & derivatives
  • Substance P / pharmacology
  • Tachykinins / pharmacology*
  • Urinary Bladder / drug effects
  • Urinary Bladder / metabolism

Substances

  • Peptide Fragments
  • Peptides, Cyclic
  • Phosphatidylinositols
  • Tachykinins
  • L 659874
  • Substance P
  • septide
  • Pyrrolidonecarboxylic Acid