contulakin G
Thr10contulakin-G
L-Leucine, 5-oxo-L-prolyl-L-seryl-L-α-glutamyl-L-α-glutamylglycylglycyl-L-seryl-L-asparaginyl-L-alanyl-O-[2-(acetylamino)-2-deoxy-3-O-β-D-galactopyranosyl-α-D-galactopyranosyl]-L-threonyl-L-lysyl-L-lysyl-L-prolyl-L-tyrosyl-L-isoleucyl-
Contulakin G is an O-glycosylated invertebrate neurotensin. Contulakin-G is a weaker agonist for the neurotensin receptor. Contulakin G is also a potent antinociceptive agent[1][2].
in vivo
Contulakin G exhibits potent analgesic activity in three pain models in rats following intrathecal delivery, namely in tail-flick (acute pain), formalin test, and CFA-induced allodynia inflammatory pain[1].
Contulakin G (0-3 nmoL, Intrathecally) significantly decreases flinching behavior in rats[2].
Contulakin G (50-500 nmoL, Intrathecally) produces a dose-dependent increase in the thermally evoked skin twitch latency by 30 min after administration in dogs[2].
Animal Model:
Male Holtzman rats (300-375 g)[2]
Dosage:
0.03, 0.1, 0.3, and 3 nmol
Administration:
Intrathecally, administered as a 10-μL bolus followed by a 10-μL saline flush
Result:
Produced a significant decrease in flinching in all phases of the formalin test in rats.
Animal Model:
Purpose-bred beagle dogs (9-12 kg)[2]
Dosage:
50, 150, or 500 nmol
Administration:
Intrathecally
Result:
Produced a dose-dependent increase in the thermally evoked skin twitch latency at 30 min after dosing in dogs, which reached statistical difference as compared to vehicle at 500 nmol.
References
[1] Lee HK, et al. A marine analgesic peptide, Contulakin-G, and neurotensin are distinct agonists for neurotensin receptors: uncovering structural determinants of desensitization properties. Front Pharmacol. 2015 Feb 10;6:11. DOI:10.3389/fphar.2015.00011 [2] Allen JW, et al. An assessment of the antinociceptive efficacy of intrathecal and epidural contulakin-G in rats and dogs. Anesth Analg. 2007 Jun;104(6):1505-13, table of contents. DOI:10.1213/01.ANE.0000219586.65112.FA
