[Mechanism of dynorphin inhibition on vasoconstriction in vitro].
Bioassay and HPLC detection were used to analyze the mechanism of inhibition of stimulation-induced vasoconstriction by dynorphin 1-13 (D1-13). Bioassay showed that D1-13 inhibited the contraction of rabbit ear artery and mesenteric artery induced by electrical field stimulation with IC50s of 8.5 +/- 1.2 x 10(-8) mol/L (n = 4) and 5.02 +/- 1.3 x 10(-7) mol/L (n = 5), respectively. D1-13 was ineffective in rabbit femoral artery at a concentration even larger than 10(-6) mol/L. D1-13 did not alter the basal tension of the blood vessel, nor the vasoconstriction induced by adding norepinephrine (NE) into the bath medium, and both constriction were markedly inhibited by phentolamine, an alpha-adrenoceptor blocker. With HPLC detection, the contents of NE in the bath medium were significantly reduced by D1-13 (5 x 10(-7) mol/L) from 340.56 +/- 73.13 pg/ml to 76.91 +/- 10.26 pg/ml as compared with control group (P less than 0.05). The effect could be completely reversed by naloxone at a concentration of 10(-6) mol/L (P less than 0.05). The results suggest that D1-13 reduces stimulation-induced vasoconstriction probably through a presynaptic inhibition of NE release from the nerve terminals.
Sun
F Y
FY
Zhang
A Z
AZ
Xia
Y
Y
D000818:Animals; D001681:Biological Assay; D002851:Chromatography, High Pressure Liquid; D004399:Dynorphins / Q000494:pharmacology*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009638:Norepinephrine / Q000378:metabolism; D010446:Peptide Fragments / Q000494:pharmacology*; D011817:Rabbits; D011957:Receptors, Opioid / Q000032:analysis; D017473:Receptors, Opioid, kappa; D014661:Vasoconstriction / Q000187:drug effects*
D010446:Peptide Fragments; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; C026843:dynorphin (1-13); D004399:Dynorphins; D009638:Norepinephrine