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SB-699,551
Systematic (IUPAC) name
3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-([(2-phenylethyl)amino]methyl)-4-biphenylyl)methyl]propanamide
Identifiers
CAS number 791789-61-2
ATC code  ?
PubChem  ?
Chemical data
Formula C 34H45N3O 
Mol. mass 511.739 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

SB-699,551 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-699,551 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]

References

  1. ^ Corbett DF, Heightman TD, Moss SF, Bromidge SM, Coggon SA, Longley MJ, Roa AM, Williams JA, Thomas DR. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorganic and Medicinal Chemistry Letters. 2005 Sep 15;15(18):4014-8. 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. 5-ht5A receptors as a therapeutic target. Pharmacology and Therapeutics. 2006 Sep;111(3):707-14. PMID 16516972
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