Chemistry:GR-196,429

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Short description: Chemical compound
GR-196,429
GR-196,429 Structure.svg
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
FormulaC14H18N2O2
Molar mass246.308 g·mol−1
3D model (JSmol)

GR-196,429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. It was one of the first synthetic melatonin agonists developed and continues to be used in scientific research, though it has never been developed for medical use. Studies in mice have shown GR-196,429 to produce both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release.[1][2][3]

References

  1. "GR196429: a nonindolic agonist at high-affinity melatonin receptors". The Journal of Pharmacology and Experimental Therapeutics 285 (3): 1239–45. June 1998. PMID 9618428. 
  2. "Pharmacological characterisation of melatonin mt1 receptor-mediated stimulation of [35S]-GTPgammaS binding". Biochemical Pharmacology 56 (9): 1167–74. November 1998. doi:10.1016/s0006-2952(98)00254-8. PMID 9802327. 
  3. "Novel non-indolic melatonin receptor agonists differentially entrain endogenous melatonin rhythm and increase its amplitude". European Journal of Pharmacology 382 (3): 157–66. October 1999. doi:10.1016/s0014-2999(99)00619-6. PMID 10556666.