一种阿片样 κ 受体 (κ-opioid receptor) 激动剂。
编号:117754
CAS号:83335-41-5
单字母:H2N-YGGFLRRQFKVVT-OH
编号: | 117754 |
中文名称: | 强啡肽B(1-13)、Dynorphin B(1-13) |
英文名: | Dynorphin B (1 - 13) |
CAS号: | 83335-41-5 |
单字母: | H2N-YGGFLRRQFKVVT-OH |
三字母: | H2N N端氨基 -Tyr酪氨酸 -Gly甘氨酸 -Gly甘氨酸 -Phe苯丙氨酸 -Leu亮氨酸 -Arg精氨酸 -Arg精氨酸 -Gln谷氨酰胺 -Phe苯丙氨酸 -Lys赖氨酸 -Val缬氨酸 -Val缬氨酸 -Thr苏氨酸 -OHC端羧基 |
氨基酸个数: | 13 |
分子式: | C74H115N21O17 |
平均分子量: | 1570.84 |
精确分子量: | 1569.88 |
等电点(PI): | - |
pH=7.0时的净电荷数: | 4.97 |
平均亲水性: | -0.4 |
疏水性值: | -0.08 |
消光系数: | 1490 |
来源: | 人工化学合成,仅限科学研究使用,不得用于人体。 |
储存条件: | 负80℃至负20℃ |
标签: | 激动剂多肽(Agonist Peptide) 强啡肽(Dynorphin) |
Dynorphin B (1-13) 是一种阿片样 κ 受体 (κ-opioid receptor) 激动剂。
Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
Definition
Dynorphins are a class of endogenous opioid peptides produced in many different parts of the brain, including the hypothalamus, the hippocampus and the spinal cord, and have many different physiological actions, depending upon the site of production.
Related peptides
Dynorphins arise from the precursor protein prodynorphin. When prodynorphin is cleaved during processing by proprotein convertase 2 (PC2), multiple active peptides are released: dynorphin A, dynorphin B, “big dynorphin” and a/ß-neo-endorphin1.
Discovery
Dynophin was discovered in the mid 1970's in the laboratory of Avram Goldstein, one of the most important researchers in the field of opioid receptors and endogenous opioid peptides. The molecular identification was achieved by Goldstein in collaboration with the Japanese biochemist, Shinro Tachibana for purification, and M. Hunkapiller and L. Hood, who performed the microsequencing.
Structural characteristics
A 4,000-dalton dynorphin (also called the “Big dynorphin”) was isolated from porcine pituitary. It has 32 amino acids, with a heptadecapeptide (17 amino acid sequence), called dynorphin A, at its amino terminus and a related tridecapeptide (13 amino acid sequence), dynorphin B, at its carboxyl terminus. The two peptides are separated by the "processing signal" Lys-Arg2.
Mechanism of action
Dynorphins primarily exert their effects through a G-protein coupled receptor called the ?-opioid receptor (KOR) 3. Although KOR is the primary receptor for all dynorphins, the peptides do have some affinity for the µ-opioid receptor (MOR), d-opioid receptor (DOR), N-methyl-D-aspartic acid (NMDA)-type glutamate receptor, and bradykinin receptor. Different dynorphins show different receptor selectivities and potencies at receptors. Both big dynorphin and dynorphin A are more potent and more selective than dynorphin B. Dynorphin decreases dopamine release by binding to KORs on dopamine nerve terminals, which leads to drug tolerance and withdrawal symptoms.
Functions
Dynorphins modulate pain response. They can significantly inhibit morphine- or beta-endorphin-induced analgesia4. Dynorphins inhibit dopamine release that would counter the pleasurable effects of cocaine5. They are important in maintaining homeostasis through appetite control and circadian rhythms6. In addition to their role in weight control, dynorphins have also been found to regulate body temperature7.
References
1. Day, R., Lazure, C., Basak, A., Boudreault, A., Limperis, P., Dong, W., et al. (1998). Prodynorphin processing by proprotein convertase 2. Cleavage at single basic residues and enhanced processing in the presence of carboxypeptidase activity. J Biol. Chem., 273(2), 829-836.
2. W Fischli, A Goldstein, M W Hunkapiller, and L E Hood (1982). Isolation and amino acid sequence analysis of a 4,000-dalton dynorphin from porcine pituitary. PNAS, 79 (17), 5435-5437.
3. Nyberg, F. & Hallburg, M. (2007). Neuropeptides in hyperthermia. Progress in brain research, 162:277-93.
4. FC Tulunay, MF Jen, JK Chang, HH Loh and NM Lee, (1981). Possible regulatory role of dynorphin on morphine- and beta-endorphin- induced analgesia. American Society for Pharmacology and Experimental Therapeutics, 219 (2), 296-298.
5. Clavin, W. (2005). Dynorphin: Nature’s Own Antidote to Cocaine (and Pleasure?).
6. Przewlocki, R., Lason, W., Konecka, A. M., Gramsch, C., Herz, A., & Reid, L. D. (1983). The opioid peptide dynorphin, circadian rhythms, and starvation. Science, 219(4580), 71-73.
7. Xin, L., Geller, E. B., & Adler, M. W. (1997). Body temperature and analgesic effects of selective mu and kappa opioid receptor agonists microdialyzed into rat brain. Journal of Pharmacology and Experimental Therapeutics, 281(1), 499-507.
DOI | 名称 | |
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10.1124/mol.112.083337 | Dynorphin--still an extraordinarily potent opioid peptide | 下载 |