SB 699551

• CAT Number: I009360
• CAS Number: 791789-61-2
• Molecular Formula: C34H45N3O
• Molecular Weight: 511.75
• Purity: ≥95%
• Synonyms: SB 699551; SB699551; SB-699551.;3-cyclopentyl-N-(2-dimethylaminoethyl)-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]propanamide
• Target: 5-ht5 Receptor Antagonist
• Solubility: Soluble in DMSO
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: 3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]propanamide
• InChI: InChI=1S/C34H45N3O/c1-36(2)24-25-37(34(38)21-16-28-10-6-7-11-28)27-31-14-19-33(20-15-31)32-17-12-30(13-18-32)26-35-23-22-29-8-4-3-5-9-29/h3-5,8-9,12-15,17-20,28,35H,6-7,10-11,16,21-27H2,1-2H3
• InChIKey: SEQAMPXQRKYYQF-UHFFFAOYSA-N
• SMILES: O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4

SB 699551 (CAT: I009360) is a selective antagonist of the 5-HT5A receptor. It acts by binding to and blocking the activity of the 5-HT5A receptor subtype, which is a member of the serotonin receptor family. By inhibiting the activation of this receptor, SB 699551 modulates the neurotransmitter signaling mediated by serotonin, specifically targeting the 5-HT5A receptor pathway. The selective antagonism of the 5-HT5A receptor may have implications in various physiological and pathological processes involving serotonin, including mood regulation, cognition, and neurological disorders.

Reference

1:Neuropharmacology. 2006 Sep;51(3):566-77. Epub 2006 Jul 17. 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.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, PMID: 16846620 DOI: 10.1016/j.neuropharm.2006.04.019
Abstract: This study utilised the selective 5-ht(5A) receptor antagonist, SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4/'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), to investigate 5-ht5A receptor function in guinea pig brain. SB-699551-A competitively antagonised 5-HT-stimulated [35S]GTPgammaS binding to membranes from human embryonic kidney (HEK293) cells transiently expressing the guinea pig 5-ht5A receptor (pA2 8.1+/-0.1) and displayed 100-fold selectivity versus the serotonin transporter and those 5-HT receptor subtypes (5-HT(1A/B/D), 5-HT2A/C and 5-HT7) reported to modulate central 5-HT neurotransmission in the guinea pig. In guinea pig dorsal raphe slices, SB-699551-A (1 microM) did not alter neuronal firing per se but attenuated the 5-CT-induced depression in serotonergic neuronal firing in a subpopulation of cells insensitive to the 5-HT1A receptor-selective antagonist WAY-100635 (100 nM). In contrast, SB-699551-A (100 or 300 nM) failed to affect both electrically-evoked 5-HT release and 5-CT-induced inhibition of evoked release measured using fast cyclic voltammetry in vitro. SB-699551-A (0.3, 1 and 3 mg/kg s.c.) did not modulate extracellular levels of 5-HT in the guinea pig frontal cortex in vivo. However, when administered in combination with WAY-100635 (0.3 mg/kg s.c.), SB-699551-A (0.3, 1 or 3 mg/kg s.c.) produced a significant increase in extracellular 5-HT levels. These studies provide evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.