KGOP01
Topic: Chemistry
From HandWiki - Reading time: 2 min
KGOP01 (H-Dmt-d-Arg-Aba-β-Ala-NH2) is a synthetic peptide derivative which acts as a potent agonist of opioid receptors and has analgesic effects.[1] It was originally derived from modification of dermorphin, a naturally occurring opioid peptide secreted by some species of South American frogs.[1]
While numerous opioid peptides are known and widely used in scientific research, such as DAMGO and DADLE, these are rapidly metabolised in the body and fail to cross the blood-brain barrier, and so do not produce centrally mediated analgesic effects.[1] KGOP01 on the other hand contains several unnatural amino acids and is both metabolically stable and able to enter the brain, resulting in potent analgesic effects in animal studies.[1]
Because it is a peptide, it can be readily hybridised with other peptide ligands and so has been widely used to produce hybrid compounds combining opioid activity with activity at receptors for neuropeptides such as nociceptin, neurokinin, neurotensin and neuropeptide FF, which may lead to the development of improved opioid analgesics with reduced side effects.[2][3][4][5][6]
See also
- Adrenorphin
- DALDA
References
- ↑ 1.0 1.1 1.2 1.3 "Mechanistic Understanding of Peptide Analogues, DALDA, [Dmt1DALDA, and KGOP01, Binding to the mu Opioid Receptor"]. Molecules 25 (9): 2087. April 2020. doi:10.3390/molecules25092087. PMID 32365707.
- ↑ "Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics". European Journal of Medicinal Chemistry 92: 64–77. March 2015. doi:10.1016/j.ejmech.2014.12.033. PMID 25544687.
- ↑ "Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain". Journal of Medicinal Chemistry 59 (8): 3777–3792. April 2016. doi:10.1021/acs.jmedchem.5b01976. PMID 27035422.
- ↑ "A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects". Pain 159 (9): 1705–1718. September 2018. doi:10.1097/j.pain.0000000000001262. PMID 29708942.
- ↑ "Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies". Journal of Medicinal Chemistry 63 (21): 12929–12941. November 2020. doi:10.1021/acs.jmedchem.0c01376. PMID 32902268.
- ↑ "Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional μ/δ-Opioid Agonist-Neurokinin Antagonist Peptidomimetics". Molecules 26 (17): 5406. September 2021. doi:10.3390/molecules26175406. PMID 34500841.
 |  |
EncycloReader
is supported by the 
KSF