[Comparison of pharmacological profile of selective kappa-opioid agonist K-II and U-50488].
K-II is an analogue of U-50488, a selective kappa-opioid agonist. Comparison of pharmacological profile of K-II and U-50488 was studied using in vitro and in vivo methods. The results showed that the IC50 values of K-II and U-50488 on electrically induced contraction of the rabbit vas deferens were 0.42 nmol/L and 26.5 nmol/L, respectively. ED50 values of K-II and U-50488 in impairing motor function of mouse in the horizontal screen test were 1.7 and 15.3 mg/kg, respectively. The effect of K-II in reducing spontaneous activity of mouse was 6 times as potent as U-50488. These results suggest that K-II is a more potent kappa agonist in pharmacological effects than U-50488.
Lu
S N
SN
Beijing Institute of Pharmacochemistry.
Ma
S C
SC
Zhang
K G
KG
Dong
Y X
YX
Cui
Y Y
YY
Li
J G
JG
Wang
C Q
CQ
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D044482:Benzeneacetamides; D005260:Female; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects*; D011758:Pyrroles / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology*; D011817:Rabbits; D014649:Vas Deferens / Q000187:drug effects
D044482:Benzeneacetamides; D011758:Pyrroles; D011759:Pyrrolidines; C052660:3,4-dichloro-N-methyl-N-(2-(1-delta(3)-pyrrolinyl)-cyclohexyl)benzeneacetamide; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer