| 词条 | 6'-Guanidinonaltrindole |
| 释义 |
| ImageFile = 6'-guanidinonaltrindole structure.png | ImageSize = 200px | IUPACName = 2-[(1S,2S,13R,21R)-22-(cyclopropylmethyl)-2,16-dihydroxy-14-oxa-11,22-diazaheptacyclo[13.9.1.01,13.02,21.04,12.05,10.019,25]pentacosa-4(12),5(10),6,8,15,17,19(25)-heptaen-8-yl]guanidine | OtherNames = |Section1={{Chembox Identifiers | CASNo = | PubChem = 9912633 | ChemSpiderID = 24674392 | ChEMBL = 610279 | SMILES = c1cc2c(cc1NC(=N)N)[nH]c3c2CC4(C5Cc6ccc(c7c6C4(C3O7)CCN5CC8CC8)O)O | StdInChI = 1S/C27H29N5O3/c28-25(29)30-15-4-5-16-17-11-27(34)20-9-14-3-6-19(33)23-21(14)26(27,7-8-32(20)12-13-1-2-13)24(35-23)22(17)31-18(16)10-15/h3-6,10,13,20,24,31,33-34H,1-2,7-9,11-12H2,(H4,28,29,30)/t20-,24+,26+,27-/m1/s1 | StdInChIKey = XDKOGAAFSBGLBO-GYHUNEDQSA-N |Section2={{Chembox Properties | C=27 | H=29 | N=5 | O=3 | Appearance = | Density = | MeltingPt = | BoilingPt = | Solubility = |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = }}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 oligomerization 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
References1. ^{{cite journal | last1 = Rives | first1 = ML | last2 = Rossillo | first2 = M | last3 = Liu-Chen | first3 = LY | last4 = Javitch | first4 = JA | year = 2012 | title = 6'-Guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment.| journal = J Biol Chem | volume = 287 | issue = 32| pages = 27050–4 | pmid = 22736766 | doi=10.1074/jbc.C112.387332 | pmc=3411045}} {{Opioidergics}}{{DEFAULTSORT:Guanidinonaltrindole, 6'-}}{{nervous-system-drug-stub}}2. ^{{cite journal |vauthors=Waldhoer M, Fong J, Jones RM, Lunzer MM, Sharma SK, Kostenis E, Portoghese PS, Whistler JL | title = A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 102 | issue = 25 | pages = 9050–5 |date=June 2005 | pmid = 15932946 | pmc = 1157030 | doi = 10.1073/pnas.0501112102 }} 3. ^1 2 3 {{cite journal|last1=Rives|first1=M.-L.|last2=Rossillo|first2=M.|last3=Liu-Chen|first3=L.-Y.|last4=Javitch|first4=J. A.|title=6'-Guanidinonaltrindole (6'-GNTI) Is a G Protein-biased -Opioid Receptor Agonist That Inhibits Arrestin Recruitment|journal=Journal of Biological Chemistry|volume=287|issue=32|year=2012|pages=27050–27054|issn=0021-9258|doi=10.1074/jbc.C112.387332|pmid=22736766|pmc=3411045}} 7 : Semisynthetic opioids|Guanidines|Indolomorphinans|Kappa agonists|Kappa antagonists|Receptor heteromer ligands|Biased ligands |
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