83397-56-2
83397-56-2 結(jié)構(gòu)式
基本信息
中文別名
N-ME-PHE(3)-嗎啡肽 英文別名
PL017TYR-PRO-(NME)PHE-DPRO-NH2
morphiceptin, N-Me-Phe(3)-
[NMPhe3,D-Pro4]morphiceptin
H-TYR-PRO-N-ME-PHE-D-PRO-NH2
[N-ME-PHE3, D-PRO4]-MORPHICEPTIN
L-Tyr-L-Pro-N-Methyl-L-Phe-D-Pro-NH2
[(NME)PHE3, DPRO4] MORPHICEPTIN, BOVINE
[NMePhe3, DPro4] b-Casomorphin: 1-4, amide, bovine
{N-METHYL-PHE3,D-PRO4}-BETA-CASOMORPHIN FRAGMENT 1-
常見問題列表
生物活性
PL-017 是一種有效的，選擇性 μ 阿片受體 (μ opioid receptor) 激動(dòng)劑，對(duì) 125I-FK 33,824 與 μ 位點(diǎn)結(jié)合的 IC50 為 5.5 nM。PL-017 在大鼠中產(chǎn)生持久的可逆性鎮(zhèn)痛作用。靶點(diǎn)
IC50: 5.5 nM ( 125 I-FK 33,824 binding to μ site)
體外研究
PL-017 has an IC 50 of 10000 nM for 125 I-DADLE binding to δ site.
體內(nèi)研究
PL-017 (0.22, 0.45, 0.9 nmol/rat; i.c.v.) has the time of maximum effect of approximately 15 to 30 mm after injection at lower doses and produces analgesia lasting as long as 4 hours with larger doses in male Sprague-Dawley rats weighing 250 to 375 g.