Chemistry:L-694247

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L-694247 is a selective serotonin 5-HT1B and 5-HT1D full agonist, with similar affinities and activational potencies at these two receptors, about 20- to 25-fold greater affinity for the serotonin 5-HT1D receptor over the serotonin 5-HT1A receptor, and negligible affinity for the serotonin 5-HT1E and 5-HT1F receptors.[1][2]

When L-694247 was injected intraventricularly in dehydrated rats, it inhibited water intake. Pre-treatment with a serotonin 5-HT1D antagonist abolished this effect. Administration of L-694,247 to normally hydrated rats had no effect on water intake.[3]

L-694247 is a 5-substituted tryptamine derivative.[4]

See also

References

  1. ↑ "How efficacious are 5-HT1B/D receptor ligands: an answer from GTP gamma S binding studies with stably transfected C6-glial cell lines". Neuropharmacology 36 (4-5): 499–512. 1997. doi:10.1016/s0028-3908(96)00170-0. PMID 9225275. 
  2. ↑ Beer, MS (November 1993). "L-694,247: a potent 5-HT1D receptor agonist.". British Journal of Pharmacology 110 (3): 1196–200. doi:10.1111/j.1476-5381.1993.tb13941.x. PMID 8298808. 
  3. ↑ CASTRO-e-SILVA, E. DE (August 1997). "Effect of Third Ventricle Administration of L-694,247, a Selective 5-HT1D Receptor Agonist, on Water Intake in Rats". Pharmacology Biochemistry and Behavior 57 (4): 749–754. doi:10.1016/S0091-3057(96)00457-1. PMID 9259002. 
  4. ↑ "2-(5-(3-(4-(Methylsulfonylamino)benzyl)-1,2,4-oxadiazol-5-yl)-1H-indole-3-yl)ethylamine". https://pubchem.ncbi.nlm.nih.gov/compound/132059. 




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