生物活性 | |||
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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 | |||
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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 |
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