Spiperon

Spiperon
(IUPAC) ime
	8-[4-(4-fluorophenyl)-4-oxo-butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
Klinički podaci
Identifikatori
CAS broj	749-02-0
ATC kod	nije dodeljen
PubChem	5265
ChemSpider	5075
UNII	4X6E73CJ0Q
KEGG	D01051
ChEMBL	CHEMBL267930
Hemijski podaci
Formula	C23H26FN3O2
Mol. masa	395.47 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H26FN3O2/c24-19-10-8-18(9-11-19)21(28)7-4-14-26-15-12-23(13-16-26)22(29)25-17-27(23)20-5-2-1-3-6-20/h1-3,5-6,8-11H,4,7,12-17H2,(H,25,29) ; Key: DKGZKTPJOSAWFA-UHFFFAOYSA-N
Farmakokinetički podaci
Metabolizam	Hepatički
Izlučivanje	Renalno
Farmakoinformacioni podaci
Trudnoća	?
Pravni status
Način primene	Oralno

Spiperon (Spiroperidol, Spiropitan) je psihoaktivni lek i istraživačkia hemikalijia koja pripada butirofenonskoj hemijskoj klasi.^[6] On funkcioniše kao antagonist 5-HT_1A, 5-HT_2A, 5-HT₇, i D₂ receptora, i bio je korišćen za identifikaciju tih receptora u obliku liganda obeleženom sa tricijumom. On ima neznatan afinitet za 5-HT_2C receptor. Osim toga, poznato je da spiperon deluje kao aktivator Ca²⁺ aktiviranih Cl^- kanala (CaCC), tako da je potencijalna meta za lečenje cistične fibroze.^[7]

N-Metilspiperon (NMSP) je derivat spiperona koji se koristi za proučavanje neurotransmiterskih sistema dopamina i serotonina. Obeležen sa radioizotopom ugljenik-11, on može da se koristi u pozitronskoj emisionoj tomografiji.^[8]

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
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ 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
↑ Zheng LT, Hwang J, Ock J, Lee MG, Lee WH, Suk K (September 2008). „The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production”. J. Neurochem. 107 (5): 1225–35. DOI:10.1111/j.1471-4159.2008.05675.x. PMID 18786164. ^{[mrtav link]}
↑ Liang L, Macdonald KD, Schwiebert EM, Zeitlin PL, Guggino WB. (October 2008). „Spiperone, Identified through Compound Screening, Activates Calcium Dependent Chloride Secretion in the Airway”. Am J Physiol Cell Physiol 296 (1): C131–41. DOI:10.1152/ajpcell.00346.2008. PMID 18987251. Arhivirano iz originala na datum 2008-12-31. Pristupljeno 2014-04-05.
↑ Bengt Andree and others (August 1998). „Positron Emission Tomographic Analysis of Dose-dependent MDL-100,907 Binding to 5-Hydroxtryptamine-2A Receptors in the Human Brain”. Journal of Clinical Psychopharmacology 18 (4): 313–323.

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

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] 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

[pmid18786164-6] Zheng LT, Hwang J, Ock J, Lee MG, Lee WH, Suk K (September 2008). „The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production”. J. Neurochem. 107 (5): 1225–35. DOI:10.1111/j.1471-4159.2008.05675.x. PMID 18786164. ^{[mrtav link]}

[pmid18987251-7] Liang L, Macdonald KD, Schwiebert EM, Zeitlin PL, Guggino WB. (October 2008). „Spiperone, Identified through Compound Screening, Activates Calcium Dependent Chloride Secretion in the Airway”. Am J Physiol Cell Physiol 296 (1): C131–41. DOI:10.1152/ajpcell.00346.2008. PMID 18987251. Arhivirano iz originala na datum 2008-12-31. Pristupljeno 2014-04-05.

[8] Bengt Andree and others (August 1998). „Positron Emission Tomographic Analysis of Dose-dependent MDL-100,907 Binding to 5-Hydroxtryptamine-2A Receptors in the Human Brain”. Journal of Clinical Psychopharmacology 18 (4): 313–323.

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