SL65.0155

SL65.0155
(IUPAC) ime
	5-(5-amino-6-hloro-2,3-dihidro-1,4-benzodioksin-8-il)-3-(1-fenetil-4-piperidil)-1,3,4-oksadiazol-2-on hidrohlorid
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	9805718
ChemSpider	7981478
Hemijski podaci
Formula	C23H26Cl2N4O4
Mol. masa	493,38 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H25ClN4O4.ClH/c24-18-14-17(20-21(19(18)25)31-13-12-30-20)22-26-28(23(29)32-22)16-7-10-27(11-8-16)9-6-15-4-2-1-3-5-15;/h1-5,14,16H,6-13,25H2;1H ; Key: LNNFXZHLRNQJIT-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SL65.0155 je selektivni parcijalni agonist 5-HT₄ receptora (K_i = 0.6 nM; IA = 40-50% (relativno na 5-HT)).^[4] On potencijalno poboljšava spoznaju, učenje, i memoriju,^[4]^[5]^[6]^[7]^[8]^[9] a poseduje i antidepresivna svojstva.^[10] SL65.0155 je bio u fazi II kliničkih ispitivanja tokom 2004-2006 za lečenje amnezije i demencije.^[11]^[12]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ ^4,0 ^4,1 Moser PC, Bergis OE, Jegham S, et al. (August 2002). „SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties”. The Journal of Pharmacology and Experimental Therapeutics 302 (2): 731-41. DOI:10.1124/jpet.102.034249. PMID 12130738.
↑ Spencer JP, Brown JT, Richardson JC, et al. (2004). „Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease”. Neuroscience 129 (1): 49-54. DOI:10.1016/j.neuroscience.2004.06.070. PMID 15489027.
↑ Micale V, Leggio GM, Mazzola C, Drago F (November 2006). „Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia”. Brain Research 1121 (1): 207-15. DOI:10.1016/j.brainres.2006.08.108. PMID 17011531.
↑ Restivo L, Roman F, Dumuis A, Bockaert J, Marchetti E, Ammassari-Teule M (September 2008). „The promnesic effect of G-protein-coupled 5-HT4 receptors activation is mediated by a potentiation of learning-induced spine growth in the mouse hippocampus”. Neuropsychopharmacology 33 (10): 2427-34. DOI:10.1038/sj.npp. 1301644. PMID 18075492.
↑ Marchetti E, Jacquet M, Jeltsch H, et al. (July 2008). „Complete recovery of olfactory associative learning by activation of 5-HT4 receptors after dentate granule cell damage in rats”. Neurobiology of Learning and Memory 90 (1): 185-91. DOI:10.1016/j.nlm.2008.03.010. PMID 18485752.
↑ Hille C, Bate S, Davis J, Gonzalez MI (December 2008). „5-HT4 receptor agonism in the five-choice serial reaction time task”. Behavioural Brain Research 195 (1): 180-6. DOI:10.1016/j.bbr.2008.08.007. PMID 18765258.
↑ Tamburella A, Micale V, Navarria A, Drago F (October 2009). „Antidepressant properties of the 5-HT4 receptor partial agonist, SL65.0155: behavioral and neurochemical studies in rats”. Progress in Neuro-psychopharmacology & Biological Psychiatry 33 (7): 1205-10. DOI:10.1016/j.pnpbp.2009.07.001. PMID 19596038.
↑ Bockaert J, Claeysen S, Compan V, Dumuis A (February 2004). „5-HT4 receptors”. Current Drug Targets. CNS and Neurological Disorders 3 (1): 39-51. PMID 14965243.
↑ Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.

Literatura

Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.

Povezano

RS-67,333

Vanjske veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[pmid12130738-4] 4,0 ^4,1 Moser PC, Bergis OE, Jegham S, et al. (August 2002). „SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties”. The Journal of Pharmacology and Experimental Therapeutics 302 (2): 731-41. DOI:10.1124/jpet.102.034249. PMID 12130738.

[pmid15489027-5] Spencer JP, Brown JT, Richardson JC, et al. (2004). „Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease”. Neuroscience 129 (1): 49-54. DOI:10.1016/j.neuroscience.2004.06.070. PMID 15489027.

[pmid17011531-6] Micale V, Leggio GM, Mazzola C, Drago F (November 2006). „Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia”. Brain Research 1121 (1): 207-15. DOI:10.1016/j.brainres.2006.08.108. PMID 17011531.

[pmid18075492-7] Restivo L, Roman F, Dumuis A, Bockaert J, Marchetti E, Ammassari-Teule M (September 2008). „The promnesic effect of G-protein-coupled 5-HT4 receptors activation is mediated by a potentiation of learning-induced spine growth in the mouse hippocampus”. Neuropsychopharmacology 33 (10): 2427-34. DOI:10.1038/sj.npp. 1301644. PMID 18075492.

[pmid18485752-8] Marchetti E, Jacquet M, Jeltsch H, et al. (July 2008). „Complete recovery of olfactory associative learning by activation of 5-HT4 receptors after dentate granule cell damage in rats”. Neurobiology of Learning and Memory 90 (1): 185-91. DOI:10.1016/j.nlm.2008.03.010. PMID 18485752.

[pmid18765258-9] Hille C, Bate S, Davis J, Gonzalez MI (December 2008). „5-HT4 receptor agonism in the five-choice serial reaction time task”. Behavioural Brain Research 195 (1): 180-6. DOI:10.1016/j.bbr.2008.08.007. PMID 18765258.

[pmid19596038-10] Tamburella A, Micale V, Navarria A, Drago F (October 2009). „Antidepressant properties of the 5-HT4 receptor partial agonist, SL65.0155: behavioral and neurochemical studies in rats”. Progress in Neuro-psychopharmacology & Biological Psychiatry 33 (7): 1205-10. DOI:10.1016/j.pnpbp.2009.07.001. PMID 19596038.

[pmid14965243-11] Bockaert J, Claeysen S, Compan V, Dumuis A (February 2004). „5-HT4 receptors”. Current Drug Targets. CNS and Neurological Disorders 3 (1): 39-51. PMID 14965243.

[isbn1-58829-568-0-12] Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.

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