CP-93129

CP-93129
Identifiers
	IUPAC name 3-(1,2,3,6-tetrahydropyridin-4-yl)-1,4-dihydropyrrolo[3,2-b]pyridin-5-one;
CAS Number	127792-75-0;
PubChem CID	124007;
IUPHAR/BPS	11;
ChemSpider	110524;
CompTox Dashboard (EPA)	DTXSID50155670 ;
Chemical and physical data
Formula	C12H13N3O
Molar mass	215.251 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C3CNCC=C3c(c1n2)cnc1ccc2=O;

CP-93129 is a drug which acts as a potent and selective serotonin 5-HT_1B receptor agonist, with approximately 150x and 200x selectivity over the closely related 5-HT_1D and 5-HT_1A receptors.[1] It is used in the study of 5-HT_1B receptors in the brain, particularly their role in modulating the release of other neurotransmitters.[2][3][4][5]

References

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.
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.
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.
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. doi:10.1152/jn.00770.2004. PMID 15716370.
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.

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[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.

[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. 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.