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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.

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If you are unable to find your desired product please contact us for assistance or send an email to info@biosyn.com

 
Product Name Catalog # Unit Price/Unit 
Biotin - Dynorphin A (1 - 17)
Biotin-YGGFLRRIRPKLKWDNQ
10936-01 1 mg $504 cart inquire
[D - Arg6] - Dynorphin A (1 - 13), porcine
YGGFLrRIRPKLK
10943-01 1 mg $675 cart inquire
[D - Arg8] - Dynorphin A (1 - 13), porcine
YGGFLRRrRPKLK
10944-01 1 mg $675 cart inquire
Deltorphin B
YaFEVVG-CONH2
10947-01 1 mg $405 cart inquire
Deltorphin C
YaFDVVG-CONH2
10946-01 1 mg $714 cart inquire
Dermorphin
YaFGYPS
10948-01 1 mg $716 cart inquire
Dynorphin A (1 - 10), porcine
YGGFLRRIRP
10941-01 1 mg $626 cart inquire
Dynorphin A (1 - 13), porcine
YGGFLRRIRPKLK
10942-01 1 mg $642 cart inquire
Dynorphin A (1 - 17)-10937-05
YGGFLRRIRPKLKWDNQ
10937-01 1 mg $801 cart inquire
Dynorphin A (1 - 7), porcine
YGGFLRR
10938-01 1 mg $593 cart inquire
Dynorphin A (1 - 8) porcine
YGGFLRRI
10939-01 1 mg $405 cart inquire
Dynorphin A (1 - 9), porcine
YGGFLRRIR
10940-01 1 mg $608 cart inquire
Dynorphin A (2 - 13), porcine
GGFLRRIRPKLK
10945-01 1 mg $642 cart inquire
Dynorphin B (1 - 13)
YGGFLRRQFKVVT
10949-01 1 mg $743 cart inquire
Dynorphin B (1 - 9)
YGGFLRRQF
10950-01 1 mg $710 cart inquire

Biosynthesis Inc.