Ziconotide Acetate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

齐考诺肽是一种镇痛剂，已用于治疗神经性和非神经性疼痛。齐考诺肽通过与位于伤害感受通路初级传入神经元末端的 N 型钙通道结合而发挥作用，从而减少突触传递，具有有效的抗伤害作用。

Ziconotide is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.

Most native cells express a variety of different calcium channels and as a result, Ziconotide acetate only partially reduces high-voltage-activated calcium currents in differentiated human neuroblastoma IMR32 cells, rat superior cervical ganglion neurons, and rat hippocampal neurons. Ziconotide acetate also reduces calcium currents that result from expression of the α1B subunit in HEK cells, tsa-201 cells, and Xenopus laevis oocytes.Ziconotide acetate delivers its antinociceptive efficacy by reducing the release of pronociceptive neurotransmitters in the dorsal horn of the spinal cord, thereby inhibiting pain signal transmission.

Ziconotide (i.t.; 25-100 pmol/site; 5 μL; on the 4 th, 10 th, 15 th, 20 th, and 24 th days) acetate reduces the levels of IL-1β and IL-23 in the CNS, as well as IL-17 production in the spleen, 25 days after MOG35-55-elicited EAE, in the mouse model of experimental autoimmune encephalomyelitis (EAE). Animal Model:Female C57BL/6mice (18-22 g, 6-8 weeks old) injected with myelin oligodendrocytes glycoprotein Dosage:25 pmol/site, 50 pmol/site, 100 pmol/site Administration:Intrathecal injection; on the 4 th, 10 th, 15 th, 20 th, and 24 th days Result:Significantly reduced the mechanical hypersensitivity in animals with EAE.

Prialt

GPCR/G Protein

Calcium Channel

Calcium Channel

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914454-03-8

2639.2

C102H172N36O32S7

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL

CC1C(=O)NC(C(=O)NC2CSSCC3C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(CSSCC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NCC(=O)N1)CCCCN)CCCCN)N)C(=O)NC(C(=O)NCC(=O)NC(C(=O)N3)CO)C(C)O)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CO)CCCNC(=N)N)CC(C)C)CCSC

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(-20℃)

With Ice Pack

≥ 2 years