[Morphine-like activity of the enkephalin analog Tyr-D-Ala-Gly-Phe-NH2].
The analgetic activity of the tetrapeptide enkephalin analog, its influence on the interneuronal transmission of excitation in various areas of the central nervous system and on opiate receptors of vas deferens were studied. The tetrapeptide was found to have a marked analgetic effect during intravenous injection to mice but to be less active than morphine. The tetrapeptide as well as morphine inhibited the impulse summation in rabbits and both spontaneous and bradykinin-induced neuronal activity in the rat sensory motor cortex. The tetrapeptide inhibited the contractions of isolated vas deferens in mice. The opiate antagonist naloxone eliminated both analgetic effect of the tetrapeptide and its inhibitory effect on the impulse summation, neuronal activity and contractions of vas deferens.
D000700:Analgesics; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects*; D004723:Endorphins / Q000494:pharmacology*; D004745:Enkephalins / Q000494:pharmacology*; D005071:Evoked Potentials / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009044:Motor Cortex / Q000187:drug effects; D010455:Peptides / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects*; D013003:Somatosensory Cortex / Q000187:drug effects; D009435:Synaptic Transmission / Q000187:drug effects; D014649:Vas Deferens / Q000187:drug effects
D000700:Analgesics; D004723:Endorphins; D004745:Enkephalins; D010455:Peptides; D011957:Receptors, Opioid; D009020:Morphine
Morfinopodobnaia aktivnost' analoga énkefalinov Tyr--D-Ala--Gly--Phe--NH2.