SB-699551

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] 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,[2] In animal studies, SB-699551 was found to block cue-mediated responding to LSD, again suggesting an antipsychotic type of activity.[3]

SB-699551
Identifiers
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC34H45N3O
Molar mass511.754 g·mol−1
3D model (JSmol)
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References

  1. {{cite journal | vauthors = 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 | display-authors = 6 | title = 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 | journal = Neuropharmacology | volume = 51 | issue = 3 | pages = 566–77 | date = September 2006 | pmid = 16846620 | doi = 10.1016/j.neuropharm.2006.04.019 }}
  2. Nikiforuk A, Hołuj M, Kos T, Popik P (June 2016). "The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia". Neuropharmacology. 105: 351–360. doi:10.1016/j.neuropharm.2016.01.035. PMID 26826431.
  3. Popik P, Krawczyk M, Kuziak A, Bugno R, Hogendorf A, Staroń J, Nikiforuk A (August 2019). "Serotonin type 5A receptor antagonists inhibit D-lysergic acid diethylamide discriminatory cue in rats". Journal of Psychopharmacology: 269881119867603. doi:10.1177/0269881119867603. PMID 31452444.
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