Antinociceptive activity of glycosidic enkephalin analogues.
The antinociceptive activity of two new enkephalin analogues: N1.5-(beta-D-glucopyranosyl)[D-Met2, Pro5]enkephalinamide and N1.5-(beta-D-galactopyranosyl)[D-Met2, Pro5]enkephalinamide was assessed using the tail immersion and paw pressure behavioural tests. Both enkephalin analogues appear to be more active than morphine when injected either into the fourth ventricle or intrathecally; the galactose analogue is more than 5000 times more active than morphine when injected into the fourth ventricle. The analgesic effects produced by the analogues are partially reversed by SC naloxone (0.1 mg/kg) and totally reversed when the dose of naloxone used was 1 mg/kg, suggesting that the analogues act upon more than one type of opiate receptor (mu/delta).
Rodríguez
R E
RE
Department of Biochemistry and Molecular Biology, Faculty of Medicine, University of Salamanca, Spain.
Rodríguez
F D
FD
Sacristán
M P
MP
Torres
J L
JL
Reig
F
F
García Antón
J M
JM
Valencia
G
G
D000700:Analgesics; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D004745:Enkephalins / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D007276:Injections, Intraventricular; D008297:Male; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D004745:Enkephalins; C056982:enkephalin, Met(2)-ProNH2(5)(N(1.5)-glucopyranosyl); C061838:enkephalinamide, Met(2)-Pro(5)-(N(1,5))-galactopyranosyl-; D009270:Naloxone; D009020:Morphine