![十大正规配资平台 [D-Arg2, Lys4]-Dermorphin (1-4) amide (DALDA);Tyr-D-Arg-Phe-Lys-NH2_搜狐网](/uploads/allimg/260211/11133QF10K05.jpg)
结构信息
一级结构:含4个氨基酸残基的线性多肽,第2位为D-精氨酸(D-Arg)取代天然强啡肽的Gly,第4位为赖氨酸(Lys)取代Pro,C端酰胺化(-NH₂),增强酶稳定性和受体结合能力。 功能位点:N端Tyr¹为阿片受体结合必需残基,D-Arg²修饰减少肽酶降解,C端酰胺化提升膜穿透性。展开剩余78%作用机理
受体选择性:特异性激动μ阿片受体(MOR),Ki值为1.69 nM,对δ、κ受体亲和力极低,是研究MOR功能的工具肽。 生物效应:激活MOR后抑制腺苷酸环化酶,降低细胞内cAMP水平,调控神经递质释放(如P物质、谷氨酸),参与疼痛感知、情绪调节及神经炎症过程。研究进展
外周镇痛模型:在慢性神经病理性疼痛动物实验中,通过皮下给药激活外周MOR发挥镇痛作用,且不产生中枢神经系统的不良反应(如成瘾、呼吸抑制)。 代谢与肾脏疾病:参与调控糖脂代谢与肾脏血流动力学,研究显示其在糖尿病肾病模型中的潜在保护作用。 药物开发:作为MOR选择性配体,用于设计新型非成瘾性镇痛药物或外周镇痛候选分子。溶解与保存
溶解:易溶于水或生理盐水,建议浓度≤10 mM,超声处理可加速溶解。 保存:冻干粉-20℃避光保存,溶解后分装于-80℃储存,避免反复冻融(建议1个月内使用)。相关多肽
[D-Ala2, D-Leu5]-Enkephalin (DADLE);Tyr-D-Ala-Gly-Phe-D-Leu [D-Ala2]-Dynorphin A (1-13) amide;Tyr-D-Ala-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-NH2 [D-Ala2]-Leu-Enkephalin-Arg (Dalargin);Tyr-D-Ala-Gly-Phe-Leu-Arg [D-Ala2]-β-Casomorphin (1-3) amide;Tyr-D-Ala-Phe-NH2 [D-Ala7]-Angiotensin I/II (1-7);Asp-Arg-Val-Tyr-Ile-His-D-Ala [D-Arg2, Lys4]-Dermorphin (1-4) amide (DALDA);Tyr-D-Arg-Phe-Lys-NH2 [D-Arg6]-Dynorphin A (1-13) ;Tyr-Gly-Gly-Phe-Leu-D-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys [D-Arg8]-Dynorphin A (1-13);Tyr-Gly-Gly-Phe-Leu-Arg-Arg-D-Arg-Arg-Pro-Lys-Leu-Lys [Deamino-Cys1, D-Tyr(Et)2, Thr4, Orn8]-Oxytocin;3-Mercaptopropionyl-D-Tyr(Et)-Ile-Thr-Asn-Cys-Pro-Orn-Gly-NH2 (Mpr1, Cys6 disulfide bridge) (Oxytocin antagonist) [des-Arg1]-Bradykinin;Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg [des-Arg9, Leu8]-Bradykinin;Arg-Pro-Pro-Gly-Phe-Ser-Pro-Leu [des-Asp1]-Angiotensin I (human);Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu [des-Gly77, des-His78]-Myelin Basic Protein (68-84) (bovine) ;Tyr-Gly-Ser-Leu-Pro-Gln-Lys-Ala-Gln-Arg-Pro-Gln-Asp-Glu-Asn [des-Gly77, des-His78]-Myelin Basic Protein (68-84) (guinea pig);Tyr-Gly-Ser-Leu-Pro-Gln-Lys-Ser-Gln-Arg-Ser-Gln-Asp-Glu-Asn、相关文献
Meyer ME, et al. DALDA (H-Tyr-D-Arg-Phe-Lys-NH₂), a potent mu-opioid peptide agonist, affects various patterns of locomotor activities. Pharmacol Biochem Behav. 1995 May;51(1):149-51. Houghten RA, et al. Synthesis and opioid activity of dermorphin analogs with D-Arg and Lys substitutions. J Med Chem. 1986;29(12):2483-2486. Chen X, et al. Peripherally acting mu-opioid receptor agonist DALDA attenuates spinal cord injury-induced pain-like behavior in mice. Pain. 2019;160(11):2643-2655.发布于:上海市联富配资提示:文章来自网络,不代表本站观点。