6'-Guanidinonaltrindole (6'-GNTI) is a κ−δ-opioid receptor selective ligand used in scientific research.[1]
With 6'-GNTI, evidence was provided for the first time that receptor oligomizeration plays functional role in living organisms.[2]
6'-GNTI is an extremely biased agonist of the κ-opioid receptor.[3] It is a potent partial agonist of the G protein pathway but does not recruit the β-arrestin pathway.[3] Due to its functional selectivity for the G protein pathway, 6'-GNTI functions as an antagonist of nonbiased KOR agonists on the β-arrestin pathway.[3] It is thought that 6'-GTNI may be able to produce analgesia without dysphoria and with a lower incidence of tolerance.[3]
See also
References
- ↑ Rives ML, Rossillo M, Liu-Chen LY, Javitch JA (2012): J Biol Chem, 287(32):27050-4. PMID 22736766
- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ 3.0 3.1 3.2 3.3 Lua error in package.lua at line 80: module 'strict' not found.
|
Receptor
(ligands) |
MOR |
|
DOR |
|
KOR |
- Agonists: 6'-GNTI
- 8-CAC
- 18-MC
- 14-Methoxymetopon
- β-Chlornaltrexamine
- β-Funaltrexamine
- Adrenorphin (metorphamide)
- Akuuamicine
- Alazocine
- Allomatrine
- Asimadoline
- BAM-12P
- BAM-18P
- BAM-22P
- Big dynorphin
- Bremazocine
- BRL-52537
- Butorphan
- Butorphanol
- BW-373U86
- Cebranopadol
- Ciprefadol
- CR665
- Cyclazocine
- Cyclorphan
- Cyprenorphine
- Diamorphine (heroin)
- Diacetylnalorphine
- Difelikefalin
- Dihydroetorphine
- Dihydromorphine
- Diprenorphine
- Dynorphin A
- Dynorphin B (rimorphin)
- Eluxadoline
- Enadoline
- Eptazocine
- Erinacine E
- Ethylketazocine
- Etorphine
- Fedotozine
- Fentanyl
- Gemazocine
- GR-89696
- GR-103545
- Hemorphin-4
- Herkinorin
- HS665
- Hydromorphone
- HZ-2
- Ibogaine
- ICI-199,441
- ICI-204,448
- Ketamine
- Ketazocine
- Laudanosine
- Leumorphin (dynorphin B-29)
- Levallorphan
- Levomethorphan
- Levorphanol
- Lexanopadol
- Lofentanil
- LPK-26
- Lufuradom
- Matrine
- MB-1C-OH
- Menthol
- Metazocine
- Metkefamide
- Mianserin
- Mirtazapine
- Morphine
- Moxazocine
- MR-2034
- N-MPPP
- Nalbuphine
- Nalbuphine sebacate
- NalBzOH
- Nalfurafine
- Nalmefene
- Nalodeine (N-allylnorcodeine)
- Nalorphine
- Naltriben
- Niravoline
- Norbuprenorphine
- Norbuprenorphine-3-glucuronide
- Noribogaine
- Norketamine
- O-Desmethyltramadol
- Oripavine
- Oxilorphan
- Oxycodone
- Pentazocine
- Pethidine (meperidine)
- Phenazocine
- Proxorphan
- Racemethorphan
- Racemorphan
- RB-64
- Salvinorin A (salvia)
- Salvinorin B ethoxymethyl ether
- Salvinorin B methoxymethyl ether
- Samidorphan
- SKF-10047
- Spiradoline (U-62,066)
- TH-030418
- Thienorphine
- Tifluadom
- Tricyclic antidepressants (e.g., amitriptyline, desipramine, imipramine, nortriptyline)
- U-50,488
- U-54,494A
- U-69,593
- Xorphanol
|
NOP |
|
Unsorted /
unknown |
|
|
Enzyme
(inhibitors) |
|
Others |
- Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)
|
|
<templatestyles src="Asbox/styles.css"></templatestyles>