CAS Number 791789-61-2 YesY
Chemical and physical data
Formula C34H45N3O
Molar mass 511.739 g/mol
3D model (Jmol) Interactive image

SB-699551 is a drug which was the first compound developed to act as a selective antagonist for the serotonin receptor 5-HT5A, with selectivity of around 100x over other serotonin receptor subtypes.[1] The function of the 5-HT5A receptor remains poorly defined, but SB-699551 was found to modulate serotonin release from neurons, suggesting it acts as a presynaptic inhibitory autoreceptor similar to the 5-HT1B and 5-HT1D receptors.[2] Multiple therapeutic roles have been suggested for 5-HT5A ligands due to the presence of this receptor in several areas of the brain, but research is still at an early stage.[3]


  1. Corbett, DF; Heightman, TD; Moss, SF; Bromidge, SM; Coggon, SA; Longley, MJ; Roa, AM; Williams, JA; Thomas, DR (2005). "Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry". Bioorganic & Medicinal Chemistry Letters. 15 (18): 4014–8. doi:10.1016/j.bmcl.2005.06.024. PMID 16002289.
  2. Thomas DR, Soffin EM, Roberts C, Kew JN, de la Flor RM, Dawson LA, Fry VA, Coggon SA, Faedo S, Hayes PD, Corbett DF, Davies CH, Hagan JJ. SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain. Neuropharmacology. 2006 Sep;51(3):566-77. PMID 16846620
  3. Thomas, DR (2006). "5-ht5A receptors as a therapeutic target". Pharmacology & therapeutics. 111 (3): 707–14. doi:10.1016/j.pharmthera.2005.12.006. PMID 16516972.

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