ANALGESIC AGENT FOR VISCERAL PAIN MANAGEMENT

摘要

FIELD: medicine.;SUBSTANCE: what is offered is application of amide N-(6-phenylhexanoyl)glycin-L-triptophane (GB-115, dipeptide, previously known as a psychotropic substance) as an agent for visceral pain management. Evident analgesic activity of the compound is shown in a visceral pain model (writhing test). An analgesic effect of GB-115 is exceeded in efficiency by morphine, nevertheless is comparable in antinociception intensity to the nonsteroidal anti-inflammatory drug diclofenac. Naltrexone iodide, a nonselective peripheral opioid receptor antagonist completely prevents GB-115 from displaying analgesic properties that testifies to GB-115 interaction with peripheral opioid receptors. The k-opioid receptor blockade by norbinaltorphimine, a selective k-receptor antagonist, arrests pharmacological effects of GB-115.;EFFECT: drug is characterised by a unique spectrum of receptor reactions and the absence of side effects, practically nontoxic, does not cause sedation and respiratory depression peculiar to opioid analgesics, does not exhibit ulcerogenic effects and action of a hematosis process inherent in NSAIDs.;6 dwg, 3 tbl