Pharmacological studies of proctolin receptors on foregut and hindgut of Blaberus craniifer

Peptides. 1998;19(10):1641-51. doi: 10.1016/s0196-9781(98)00120-x.

Abstract

Proctolin (Arg-Tyr-Leu-Pro-Thr) and proctolin analogs modified at position 1, 2, or 5 caused dose dependent contractions of Blaberus fore- and hindgut. The varying contractile effects between both tissues revealed the possible presence of receptor subtypes as identified by [GABA1]-proctolin. A single population of binding sites (Kd approximately 100 nM) was deduced from Scatchard analysis. In addition, nanomolar concentrations of proctolin induced a dose-dependent hydrolysis of phosphoinositides (PIns) augmented by GTPgammaS (1 microM) on foregut membranes but no accumulation of cAMP. Proctolin induced contractions are likely mediated via a phospholipase C linked to a heptahelical receptor bound to heterotrimeric G-proteins.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Cell Membrane / chemistry
  • Cell Membrane / drug effects
  • Cell Membrane / enzymology
  • Cockroaches
  • Cyclic AMP / metabolism
  • Dose-Response Relationship, Drug
  • Hydrolysis / drug effects
  • Neuropeptides*
  • Neurotransmitter Agents / pharmacology*
  • Oligopeptides / pharmacology*
  • Phosphatidylinositols / metabolism
  • Protein Binding / drug effects
  • Receptors, Neuropeptide / classification
  • Receptors, Neuropeptide / metabolism*
  • Receptors, Neuropeptide / physiology
  • Second Messenger Systems / drug effects
  • Stomach / chemistry*
  • Stomach / cytology
  • Stomach / drug effects

Substances

  • Neuropeptides
  • Neurotransmitter Agents
  • Oligopeptides
  • Phosphatidylinositols
  • Receptors, Neuropeptide
  • proctolin
  • Cyclic AMP
  • Adenylyl Cyclases