6'-Guanidinonaltrindole

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6'-Guanidinonaltrindole
6'-guanidinonaltrindole structure.png
Properties
C27H29N5O3
Molar mass 471.56 g·mol−1
Vapor pressure {{{value}}}
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references

6'-Guanidinonaltrindole (6'-GNTI) is a κδ-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

  1. Rives ML, Rossillo M, Liu-Chen LY, Javitch JA (2012): J Biol Chem, 287(32):27050-4. PMID 22736766
  2. Lua error in package.lua at line 80: module 'strict' not found.
  3. 3.0 3.1 3.2 3.3 Lua error in package.lua at line 80: module 'strict' not found.


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