SB-699,551

SB-699,551
(IUPAC) ime
	3-ciklopentil-N-[2-(dimetilamino)etil]-N-[(4'-([(2-feniletil)amino]metil)-4-bifenilil)metil]propanamid
Klinički podaci
Identifikatori
CAS broj	791789-61-2
ATC kod	nije dodeljen
Hemijski podaci
Formula	C34H45N3O
Mol. masa	511,739 g/mol
SMILES	eMolekuli & PubHem
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 ; Key: SEQAMPXQRKYYQF-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

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] ^[2]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.^[3] 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.^[4]

Reference[uredi | uredi kod]

↑ Corbett, DF; Heightman, TD; Moss, SF; Bromidge, SM; Coggon, SA; Longley, MJ; Roa, AM; Williams, JA i 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.
↑ [|Tocris]. „SB 699551”.
↑ 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. DOI:10.1016/j.pharmthera.2005.12.006. PMID 16516972.

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[1] Corbett, DF; Heightman, TD; Moss, SF; Bromidge, SM; Coggon, SA; Longley, MJ; Roa, AM; Williams, JA i 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] [|Tocris]. „SB 699551”.

[3] 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

[4] 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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SB-699,551

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