Org 27569

Org 27569
(IUPAC) ime
	5-hloro-3-etil-1H-indol-2-karboksilna kiselina [2-(4-piperidin-1-il-fenil)etil]amid
Klinički podaci
Identifikatori
CAS broj	868273-06-7
ATC kod	nije dodeljen
PubChem	44828492
ChemSpider	22369629
Hemijski podaci
Formula	C24H28ClN3O
Mol. masa	409,951 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C24H28ClN3O/c1-2-20-21-16-18(25)8-11-22(21)27-23(20)24(29)26-13-12-17-6-9-19(10-7-17)28-14-4-3-5-15-28/h6-11,16,27H,2-5,12-15H2,1H3,(H,26,29) ; Key: AHFZDNYNXFMRFQ-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Org 27569 je lek koji deluje kao potentan i selektivan alosterini modulator kanabinoidnog CB₁ receptor. In vitro ispitivanja sugerišu da se vezuje za regulatorno mesto na CB₁ receptoru, čime uzrokuje konformacionu promenu koja povećava afinitet vezivanja CB₁ agonista poput CP 55,940, dok umanjuje afinitet vezivanja CB₁ antagonista ili inverznih agonista poput rimonabanta. Međutim dok Org 27569 povećava sposobnost CB₁ agonista da se veži za receptor, on umanjuje efikasnost stimulacije signalizacije sekundarnim glasnikom, tako da se u praksi ponaša kao nepremostiv antagonist funkcije CB₁ receptora.^[4]

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
↑ Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, Pertwee RG, Ross RA (November 2005). „Allosteric modulation of the cannabinoid CB1 receptor”. Molecular Pharmacology 68 (5): 1484–95. DOI:10.1124/mol.105.016162. PMID 16113085.

Spoljašnje 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

[pmid16113085-4] Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, Pertwee RG, Ross RA (November 2005). „Allosteric modulation of the cannabinoid CB1 receptor”. Molecular Pharmacology 68 (5): 1484–95. DOI:10.1124/mol.105.016162. PMID 16113085.

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