[Modulating effect of cerulein on benzodiazepine receptors].

Abstract

Subcutaneous administration of caerulein (100-500 micrograms/kg) significantly reduced the development of picrotoxin (8 mg/kg) seizures in male mice. The same doses of caerulein inhibited 3H-flunitrazepam binding in in vivo experiments. Proglumide, an antagonist of cholecystokinin receptors, in low dose (5 mg/kg) potentiated the effects of caerulein (100 micrograms/kg), whereas the administration of proglumide in high dose (25 mg/kg) reduced the action of caerulein on 3H-flunitrazepam binding and picrotoxin seizures. Caerulein (5-1000 nM) decreased 3H-flunitrazepam binding in in vitro experiments only after supplementation of the binding medium with 120 mM NaCl and 5mM KCl. The results suggest the possible interaction of caerulein with chloride ionophor. It seems probable that the direct interaction of caerulein with chloride ionophor in involved in the inhibitory effect of caerulein on picrotoxin seizures and 3H-flunitrazepam binding.

• Authors: E E Vasar, L K Riago, A Kh Soosaar, A M Nurk, M O Maĭmets
• Journal: Biulleten' eksperimental'noi biologii i meditsiny (Biull Eksp Biol Med) Vol. 100 Issue 12 Pg. 711-3 (Dec 1985) ISSN: 0365-9615 [Print] Russia (Federation)
• Vernacular Title: Moduliruiushchee vliianie tseruleina na benzodiazepinovye retseptory.
• PMID: 3000472 (Publication Type: English Abstract, Journal Article)

Chemical References

• Receptors, GABA-A
• Picrotoxin
• Flunitrazepam
• Ceruletide
• Proglumide

Topics

• Animals
• Brain (drug effects, metabolism)
• Ceruletide (pharmacology)
• Dose-Response Relationship, Drug
• Drug Interactions
• Flunitrazepam (metabolism)
• Male
• Mice
• Picrotoxin (toxicity)
• Proglumide (pharmacology)
• Reaction Time (drug effects)
• Receptors, GABA-A (drug effects, metabolism)
• Seizures (chemically induced)