| 规格: | 98% |
| 分子量: | 1062.3 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
Background:
CTOP is a peptide antagonist of the μ-opioid receptor (IC50 = 2.8 nM).1 It is selective for μ-opioid receptors over δ-opioid receptors (IC50 = 13,500 nM) and somatostatin receptors (IC50 = 24,000 nM). CTOP inhibits the antinociceptive effect of morphine in the tail flick test in mice (ED50 = 0.018 nmol) and reverses morphine-induced increases in locomotor activity (ED50 = 0.02 nmol).2 It also induces withdrawal symptoms in a mouse model of chronic, but not acute, morphine dependence.
参考文献
1. Pelton, J.T., Kazmierski, W., Gluya, K., et al. Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. Journal of Medicinal Chemistry 29(11), 2370-2375 (2013).
2. Gulya, K., KrivÁn, M., Nyolczas, N., et al. Central effects of the potent and highly selective μ opioid antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) in mice. Eur. J. Pharmacol. 150(3), 355-360 (1988).
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