SB-699,551

SB-699,551
IUPAC ime
	3-ciklopentil-N-[2-(dimetilamino)etil]-N-[(4'-([(2-feniletil)amino]metil)-4-bifenilil)metil]propanamid
Identifikatori
CAS broj	791789-61-2
ATC kod	none
Hemijski podaci
Formula	C34H45N3O
Molarna masa	511,739 g/mol
	SMILES C2CCCC2CCC(=O)N(CCN(C)C)Cc(cc3)ccc3-c(cc1)ccc1CNCCc4ccccc4; ;

SB-699,551 je lek koji je bio prvo jedinjenje razvijeno da deluje kao selektivni antagonist za serotoninski receptor 5-HT_5A, sa selektivnošću od oko 100x u odnosu na druge serotoninske receptor.^[1] Funkcija 5-HT_5A receptora nije potpuno izučena. Utvrđeno je da SB-699,551 moduliše otpuštanje serotonina iz neurona, te sledi da ovaj receptor deluje kao presinaptički inhibitorni autoreceptor slično 5-HT_1B i 5-HT_1D receptorima.^[2] Vešestruke terapeutske uloge su predložene za 5-HT_5A ligande usled prisustva ovog receptora u nekoliko oblasti mozga, ali su istraživanja još uvek u ranom stupnju.^[3]

Reference

^ 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. PMID 16002289. doi:10.1016/j.bmcl.2005.06.024.
^ 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]methyl4-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
^ Thomas, DR (2006). „5-ht5A receptors as a therapeutic target”. Pharmacology & therapeutics. 111 (3): 707—14. PMID 16516972. doi:10.1016/j.pharmthera.2005.12.006.

Spoljašnje veze

[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. PMID 16002289. doi:10.1016/j.bmcl.2005.06.024.

[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]methyl4-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. PMID 16516972. doi:10.1016/j.pharmthera.2005.12.006.

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