CP-93129

Summary

CP-93129 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 150x and 200x selectivity over the closely related 5-HT1D and 5-HT1A receptors.[1] It is used in the study of 5-HT1B receptors in the brain, particularly their role in modulating the release of other neurotransmitters.[2][3][4][5]

CP-93129
Identifiers
  • 3-(1,2,3,6-tetrahydropyridin-4-yl)-1,4-dihydropyrrolo[3,2-b]pyridin-5-one
CAS Number
  • 127792-75-0 checkY
PubChem CID
  • 124007
IUPHAR/BPS
  • 11
ChemSpider
  • 110524
UNII
  • Y4BW369LGS
CompTox Dashboard (EPA)
  • DTXSID50155670 Edit this at Wikidata
Chemical and physical data
FormulaC12H13N3O
Molar mass215.256 g·mol−1
3D model (JSmol)
  • Interactive image
  • C3CNCC=C3c(c1n2)cnc1ccc2=O

References edit

  1. ^ Macor JE, Burkhart CA, Heym JH, Ives JL, Lebel LA, Newman ME, et al. (August 1990). "3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole". Journal of Medicinal Chemistry. 33 (8): 2087–93. doi:10.1021/jm00170a007. PMID 2374139.
  2. ^ De Groote L, Olivier B, Westenberg HG (August 2003). "Role of 5-HT1B receptors in the regulation of extracellular serotonin and dopamine in the dorsal striatum of mice". European Journal of Pharmacology. 476 (1–2): 71–7. doi:10.1016/s0014-2999(03)02154-x. PMID 12969751.
  3. ^ Przegaliński E, Papla I, Siwanowicz J, Filip M (May 2004). "Effects of 5-HT1B receptor ligands microinjected into the ventral tegmental area on the locomotor and sensitizating effects of cocaine in rats". European Neuropsychopharmacology. 14 (3): 217–25. doi:10.1016/S0924-977X(03)00106-8. PMID 15056481. S2CID 308992.
  4. ^ Bramley JR, Sollars PJ, Pickard GE, Dudek FE (June 2005). "5-HT1B receptor-mediated presynaptic inhibition of GABA release in the suprachiasmatic nucleus". Journal of Neurophysiology. 93 (6): 3157–64. CiteSeerX 10.1.1.325.6052. doi:10.1152/jn.00770.2004. PMID 15716370.
  5. ^ Saitow F, Murano M, Suzuki H (March 2009). "Modulatory effects of serotonin on GABAergic synaptic transmission and membrane properties in the deep cerebellar nuclei". Journal of Neurophysiology. 101 (3): 1361–74. doi:10.1152/jn.90750.2008. PMID 19144744.