A-349,821

A-349,821
(IUPAC) ime
	(4'-[3-(2R,5R-dimetilpirolidin-1-il)propoksi]bifenil-4-il)morfolin-4-ilmetanon
Klinički podaci
Identifikatori
CAS broj	372513-99-0
ATC kod	nije dodeljen
PubChem	9954017
ChemSpider	8129627
ChEMBL	CHEMBL179702
Hemijski podaci
Formula	C26H34N2O3
Mol. masa	422,558
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C26H34N2O3/c1-20-4-5-21(2)28(20)14-3-17-31-25-12-10-23(11-13-25)22-6-8-24(9-7-22)26(29)27-15-18-30-19-16-27/h6-13,20-21H,3-5,14-19H2,1-2H3/t20-,21-/m1/s1 ; Key: CFUHKRLMDNFZED-NHCUHLMSSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

A-349,821 je potentan i selektivan antagonist histaminskog H₃ receptora^[5] (a verovatno i inverzni agonist).^[6] Pokazano je da ima nootropno dejstvo u životinjskim studijama.^[7] Ovo jedinjenje se koristi u laboratorijskim istraživanjima.

Reference uredi

↑ 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
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Faghih, R; Dwight, W; Pan, JB; Fox, GB; Krueger, KM; Esbenshade, TA; McVey, JM; Marsh, K i dr.. (2003). „Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists”. Bioorganic & Medicinal Chemistry Letters 13 (7): 1325–8. DOI:10.1016/S0960-894X(03)00118-5. PMID 12657274.
↑ Witte, DG; Yao, BB; Miller, TR; Carr, TL; Cassar, S; Sharma, R; Faghih, R; Surber, BW i dr.. (2006). „Detection of multiple H3 receptor affinity states utilizing 3HA-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand”. British Journal of Pharmacology 148 (5): 657–70. DOI:10.1038/sj.bjp.0706752. PMC 1751875. PMID 16715122.
↑ Esbenshade, TA; Fox, GB; Krueger, KM; Baranowski, JL; Miller, TR; Kang, CH; Denny, LI; Witte, DG i dr.. (2004). „Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist”. Biochemical pharmacology 68 (5): 933–45. DOI:10.1016/j.bcp.2004.05.048. PMID 15294456.

Vidi još uredi

Antagonist H3 receptora

[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

[4] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[5] Faghih, R; Dwight, W; Pan, JB; Fox, GB; Krueger, KM; Esbenshade, TA; McVey, JM; Marsh, K i dr.. (2003). „Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists”. Bioorganic & Medicinal Chemistry Letters 13 (7): 1325–8. DOI:10.1016/S0960-894X(03)00118-5. PMID 12657274.

[6] Witte, DG; Yao, BB; Miller, TR; Carr, TL; Cassar, S; Sharma, R; Faghih, R; Surber, BW i dr.. (2006). „Detection of multiple H3 receptor affinity states utilizing 3HA-349821, a novel, selective, non-imidazole histamine H3 receptor inverse agonist radioligand”. British Journal of Pharmacology 148 (5): 657–70. DOI:10.1038/sj.bjp.0706752. PMC 1751875. PMID 16715122.

[7] Esbenshade, TA; Fox, GB; Krueger, KM; Baranowski, JL; Miller, TR; Kang, CH; Denny, LI; Witte, DG i dr.. (2004). „Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist”. Biochemical pharmacology 68 (5): 933–45. DOI:10.1016/j.bcp.2004.05.048. PMID 15294456.

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