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Porcine dynorphin A (1-13) 是一个有效的内源性阿片受体 (κ opioid receptor) 激动剂，在生理浓度下它有镇痛作用。

Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.

Porcine dynorphin A(1-13) acetate是一种内源性阿片肽，优先激活κ阿片受体。

Porcine dynorphin A(1-13) acetate is an endogenous opioid peptide that preferentially activates κ opioid receptors.

Peptide H-YGGFLRRIRPKLK-OH is a Research Peptide with significant interest within the field academic and medical research. Recent citations using H-YGGFLRRIRPKLK-OH include the following: A serine protease from suspension-cultured soybean cells ZJ Guo, C Lamb, RA Dixon - Phytochemistry, 1998 - Elsevierhttps://www.sciencedirect.com/science/article/pii/S003194229700441X Molecular mechanism of opioid receptor selection R Schwyzer - Biochemistry, 1986 - ACS Publicationshttps://pubs.acs.org/doi/pdf/10.1021/bi00368a075 Rational design of peptide ligands for the kappa opioid receptor MJ Przydzial - 2005 - search.proquest.comhttps://search.proquest.com/openview/69d929b4fdb3bcc3338b3381625a128b/1?pq-origsite=gscholar&cbl=18750&diss=y Enzymatic properties of venoms from Brazilian scorpions of Tityus genus and the neutralisation potential of therapeutical antivenoms EJ Venancio , FCV Portaro , AK Kuniyoshi, DC Carvalho - Toxicon, 2013 - Elsevierhttps://www.sciencedirect.com/science/article/pii/S0041010113000822 Side Chain Cleavage in TEMPO-assisted Free Radical Initiated Peptide Sequencing (FRIPS): Amino Acid Composition Information# CS Lee, I Jang, S Hwangbo, B Moon - Bulletin of the Korean , 2015 - Wiley Online Libraryhttps://onlinelibrary.wiley.com/doi/abs/10.1002/bkcs.10150 Identification of a plant aminopeptidase with preference for aromatic amino acid residues as a novel member of the prolyl oligopeptidase family of serine proteases A Tsuji, Y Fujisawa, T Mino - The journal of , 2011 - academic.oup.comhttps://academic.oup.com/jb/article-abstract/150/5/525/827169 High-Throughput Synthesis of Peptide alpha-Thioesters: A Safety Catch Linker Approach Enabling Parallel Hydrogen Fluoride Cleavage A Brust , CI Schroeder , PF Alewood - ChemMedChem, 2014 - Wiley Online Libraryhttps://chemistry-europe.onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201300524

As a dynorphin peptide, Dynorphin A has affinity for opioid receptors in particular it favors kappa-opioid receptors and residues 1-13 of the Dynorphin A peptide are crucial for its potency. Kappa-opioid receptors are expressed in the brain, peripheral tissues and the spinal cord and are located in areas involved in pain. For example when Dynorphin A binds to kappa-opioid receptors, dopamine is inhibited in areas of the brain prevalent in drug addiction, thus demonstrated Dynorphin A to have antagonistic effects on the brain reward circuit. Dynorphin A could be a useful research tool for studying analgesia, reward and addiction.\nThis product is available as a 0.5mg vial.

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.