GR-89696
Chemical compound
Identifiers | |
---|---|
| |
CAS Number |
|
PubChem CID |
|
IUPHAR/BPS |
|
ChemSpider |
|
UNII |
|
ChEMBL |
|
PDB ligand |
|
CompTox Dashboard (EPA) |
|
Chemical and physical data | |
Formula | C19H25Cl2N3O3 |
Molar mass | 414.33 g·mol−1 |
3D model (JSmol) |
|
| |
InChI
| |
NY (what is this?) (verify) |
GR-89696 is a drug which acts as a highly selective κ-opioid agonist.[1] It has been studied in various animal species, and has been described as selective for the κ2 subtype.[2][3][4] Recent studies have suggested that GR-89696 and related κ2-selective agonists may be useful for preventing the itching which is a common side effect of conventional opioid analgesic drugs, without the additional side effects of non-selective kappa agonists.[5] The structure bound to the κ-opioid receptor has been reported.[6]
References
- ^ Naylor A, Judd DB, Lloyd JE, Scopes DI, Hayes AG, Birch PJ (July 1993). "A potent new class of kappa-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines". Journal of Medicinal Chemistry. 36 (15): 2075–2083. doi:10.1021/jm00067a004. PMID 8393489.
- ^ Herrero JF, Headley PM (September 1993). "Functional evidence for multiple receptor activation by kappa-ligands in the inhibition of spinal nociceptive reflexes in the rat". British Journal of Pharmacology. 110 (1): 303–309. doi:10.1111/j.1476-5381.1993.tb13809.x. PMC 2176008. PMID 8220893.
- ^ Ho J, Mannes AJ, Dubner R, Caudle RM (April 1997). "Putative kappa-2 opioid agonists are antihyperalgesic in a rat model of inflammation". The Journal of Pharmacology and Experimental Therapeutics. 281 (1): 136–141. PMID 9103490.
- ^ Butelman ER, Ko MC, Traynor JR, Vivian JA, Kreek MJ, Woods JH (September 2001). "GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics. 298 (3): 1049–1059. PMID 11504802.
- ^ Ko MC, Husbands SM (January 2009). "Effects of atypical kappa-opioid receptor agonists on intrathecal morphine-induced itch and analgesia in primates". The Journal of Pharmacology and Experimental Therapeutics. 328 (1): 193–200. doi:10.1124/jpet.108.143925. PMC 2719014. PMID 18842704.
- ^ Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, et al. (May 2023). "Ligand and G-protein selectivity in the κ-opioid receptor". Nature. 617 (7960): 417–425. Bibcode:2023Natur.617..417H. doi:10.1038/s41586-023-06030-7. PMC 10172140. PMID 37138078.
- v
- t
- e
(MOR)
(DOR)
(KOR)
(NOP)
Agonists |
|
---|---|
Antagonists |
|
- Enkephalinase inhibitors: Amastatin
- BL-2401
- Candoxatril
- D -Phenylalanine
- Dexecadotril (retorphan)
- Ecadotril (sinorphan)
- Kelatorphan
- Racecadotril (acetorphan)
- RB-101
- RB-120
- RB-3007
- Opiorphan
- Selank
- Semax
- Spinorphin
- Thiorphan
- Tynorphin
- Ubenimex (bestatin)
- Propeptides: β-Lipotropin (proendorphin)
- Prodynorphin
- Proenkephalin
- Pronociceptin
- Proopiomelanocortin (POMC)
- Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)
This analgesic-related article is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e