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, Nielsen JA, Ryan K, Schulz DW, Torgersen LK, et al. 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. 1990 Aug;33(8):2087-93. PMID 2374139
^ De Groote L, Olivier B, Westenberg HG. Role of 5-HT1B receptors in the regulation of extracellular serotonin and dopamine in the dorsal striatum of mice. European Journal of Pharmacology. 2003 Aug 22;476(1-2):71-7. PMID 12969751
^ Przegaliński E, Papla I, Siwanowicz J, Filip M. Effects of 5-HT1B receptor ligands microinjected into the ventral tegmental area on the locomotor and sensitizating effects of cocaine in rats. European Neuropsychopharmacology. 2004 May;14(3):217-25. PMID 15056481
^ Bramley JR, Sollars PJ, Pickard GE, Dudek FE. 5-HT1B receptor-mediated presynaptic inhibition of GABA release in the suprachiasmatic nucleus. Journal of Neurophysiology. 2005 Jun;93(6):3157-64. PMID 15716370
^ Saitow F, Murano M, Suzuki H. Modulatory effects of serotonin on GABAergic synaptic transmission and membrane properties in the deep cerebellar nuclei. Journal of Neurophysiology. 2009 Mar;101(3):1361-74. PMID 19144744

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[1] Macor JE, Burkhart CA, Heym JH, Ives JL, Lebel LA, Newman ME, Nielsen JA, Ryan K, Schulz DW, Torgersen LK, et al. 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. 1990 Aug;33(8):2087-93. PMID 2374139

[2] De Groote L, Olivier B, Westenberg HG. Role of 5-HT1B receptors in the regulation of extracellular serotonin and dopamine in the dorsal striatum of mice. European Journal of Pharmacology. 2003 Aug 22;476(1-2):71-7. PMID 12969751

[3] Przegaliński E, Papla I, Siwanowicz J, Filip M. Effects of 5-HT1B receptor ligands microinjected into the ventral tegmental area on the locomotor and sensitizating effects of cocaine in rats. European Neuropsychopharmacology. 2004 May;14(3):217-25. PMID 15056481

[4] Bramley JR, Sollars PJ, Pickard GE, Dudek FE. 5-HT1B receptor-mediated presynaptic inhibition of GABA release in the suprachiasmatic nucleus. Journal of Neurophysiology. 2005 Jun;93(6):3157-64. PMID 15716370

[5] Saitow F, Murano M, Suzuki H. Modulatory effects of serotonin on GABAergic synaptic transmission and membrane properties in the deep cerebellar nuclei. Journal of Neurophysiology. 2009 Mar;101(3):1361-74. PMID 19144744

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