Rat CGRP-(8-37) TFA salt

产品说明书

Print
Chemical Structure| N/A 同义名 : -
CAS号 : N/A
货号 : A1159618
分子式 : C140H225F3N42O43
纯度 : 98%
分子量 : 3241.54
MDL号 : N/A
存储条件:

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Rat CGRP-(8-37) TFA salt, a cholestanol-conjugated antagonist, accumulated in CLR(calcitonin receptor-like receptor)-containing endosomes and selectively inhibited CLR signaling in endosomes. CGRP8-37-cholestanol, but not unconjugated CGRP8-37, prevented sustained neuronal excitation. When injected intrathecally to mice, CGRP8-37-cholestanol inhibited nociceptive responses to intraplantar injection of capsaicin, formalin, or complete Freund's adjuvant more effectively than unconjugated CGRP8-37[3]. CGRP(8-37) is a truncated version of calcitonin gene-related peptide (CGRP) that binds to the CGRP receptor with similar affinity but does not activate the receptor and is a highly selective CGRP receptor antagonist. CGRP-(8-37) is effective in alleviating mechanical and thermal allodynia in a dose-dependent manner. The 50 nM dose is most efficacious for both forelimb and hindlimb responses. The period of efficacy is 10 min to onset for a duration of 20 min[4]. Intrathecal administration of 5 nmol or 10 nmol of CGRP-(8-37), but not 1 nmol, induces a significant increase in hindpaw withdrawal latency. Intrathecal administration of CGRP-(8-37) not only reverses the SP-induced decrease in latency to both withdrawal responses but also mediates a significant increase in response latency compared to basal levels[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.31mL

0.06mL

0.03mL

1.54mL

0.31mL

0.15mL

3.08mL

0.62mL

0.31mL

参考文献

[1]Bennett AD, et al. Alleviation of mechanical and thermal allodynia by CGRP(8-37) in a rodent model of chroniccentral pain. Pain. 2000 May;86(1-2):163-75.

[2]Yu LC, et al. The calcitonin gene-related peptide antagonist CGRP8-37 increases the latency to withdrawalresponses in rats. Brain Res. 1994 Aug 8;653(1-2):223-30.

[3]Yarwood RE, Imlach WL, Lieu T, et al. Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission. Proc Natl Acad Sci U S A. 2017;114(46):12309‐12314

[4]Bennett AD, Chastain KM, Hulsebosch CE. Alleviation of mechanical and thermal allodynia by CGRP(8-37) in a rodent model of chronic central pain. Pain. 2000;86(1-2):163‐175

[5]Yu LC, Hansson P, Lundeberg T. The calcitonin gene-related peptide antagonist CGRP8-37 increases the latency to withdrawal responses in rats [published correction appears in Brain Res 1994 Dec 15;666(2):295]. Brain Res. 1994;653(1-2):223‐230