Tioperamid

Tioperamid
(IUPAC) ime
	N-Cikloheksil-4-(1H-imidazol-4-il)piperidin-1-karbotioamid
Klinički podaci
Identifikatori
CAS broj	106243-16-7
ATC kod	nije dodeljen
PubChem	3035905
ChemSpider	2300031
ChEMBL	CHEMBL260374
Hemijski podaci
Formula	C15H24N4S
Mol. masa	292,44 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C15H24N4S/c20-15(18-13-4-2-1-3-5-13)19-8-6-12(7-9-19)14-10-16-11-17-14/h10-13H,1-9H2,(H,16,17)(H,18,20) ; Key: QKDDJDBFONZGBW-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Tioperamid je potentan i selektivan antagonist histaminskog H₃ receptora, koji ima sposobnost prolaza kroz krvno-moždanu barijeru.

Tioperamid je korišten u ranim ekperimentima sa H3 receptorom.^[5] Utvrđeno je da je tioperamid antagonist histaminskih autoreceptora, koji detektuju prisustvo histamina. Tioperamid pojačava aktivnost histaminergičkih neurona putem blokiranja autoreceptora, čime se sprečava detekcija histamina neuronima. Posledica toga je da neuroni otpuštaju više histamina.

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
↑ 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
↑ Schwartz, Jean-Charles. The histamine H3 receptor: from discovery to clincial trials with pitolisant. BPJ 2011 May Abstract

Povezano

Antihistaminik

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

[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] Schwartz, Jean-Charles. The histamine H3 receptor: from discovery to clincial trials with pitolisant. BPJ 2011 May Abstract

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