产品
编 号:F059522
分子式:C30H45N9O5
分子量:611.74
产品类型
结构图
CAS No: 118476-85-0
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产品详情
生物活性:
DALDA is a potent and highly selective μ-opioid receptor agonist with a Ki of 1.69 nM. DALDA shows antinociceptive and respiratory effects.
体内研究:
DALDA (0-7 nmol/rat; i.t.; once) 在大鼠中表现出抗痛和呼吸作用。DALDA (0.1 and 1.0 μg/side; ICV; once) 在大鼠中产生双相效应,初始抑制,中间显著抑制,接着是水平运动、饲养和刻板印象次数的激活。Animal Model:Male Sprague-Dawley rats (300–350 g)
Dosage:0.24, 0.7 and 7 nmol/rat
Administration:Intrathecal injection, once
Result:Showed antinociceptive effects with an ED50 of 237 pmol/rat in the rat tail-flick test. Inhibited the uptake of NE in spinal cord synaptosomes in a dose-dependent manner. Had no effect on 5-HT uptake. Produced depression in minute ventilation.
Animal Model:Male Long-Evans rats, weighing 200-225 g
Dosage:0, 0.1 and 1.0 μg/side, 0.5 μL
Administration:Lateral cerebral ventricle injection, once
Result:Elicited a significant biphasic effect with an initial suppression, an intermediate marked inhibition, followed by significant activation for horizontal movement time, rearing time, and stereotypy time.
体外研究:
DALDA 在生理 pH 值下携带净正电荷 (3+),因此是亲水的,比吗啡更极性。