Proksifan

Proksifan
Nazivi
	IUPAC naziv 4-[3-(benzyloxy)propyl]-1H-imidazole
	Drugi nazivi 5-[3-(benzyloxy)propyl]-1H-imidazole
Identifikacija
CAS broj	177708-09-7;
3D model (Jmol)	interaktivna slika;
ChemSpider	4927056;
IUPHAR/BPS	1255;
PubChem C ID	6421522;
	SMILES C1=CC=C(C=C1)COCCCC2=CN=CN2; ; ; ; ; ;
Svojstva
Hemijska formula	C13H16N2O
Molarna masa	216,279 g/mol
	Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa).
	Reference infokutije

Proksifan je ligand histaminskog H₃ receptora, koji je „proteanski agonist“. On proizvodi različite efekte u opsegu od punog agonista do antagonista, do inverznog agonista u različitim tkivima, u zavisnosti od nivoa konstitutivne aktivnosti histaminskog H3 receptora. To mu daje kompleksan profil aktivnosti in vivo.^[3]^[4]^[5]^[6]^[7]^[8]^[9]

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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди
^ 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.
^ Morisset, S.; Rouleau, A.; Ligneau, X.; Gbahou, F.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2000). „High constitutive activity of native H3 receptors regulates histamine neurons in brain”. Nature. 408 (6814): 860—864. PMID 11130725. S2CID 4391762. doi:10.1038/35048583.
^ Fox, G. B.; Pan, J. B.; Esbenshade, T. A.; Bitner, R. S.; Nikkel, A. L.; Miller, T.; Kang, C. H.; Bennani, Y. L.; Black, L. A.; Faghih, R.; Hancock, A. A.; Decker, M. W. (2002). „Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model”. Pharmacology, Biochemistry, and Behavior. 72 (3): 741—750. PMID 12175472. S2CID 45861589. doi:10.1016/s0091-3057(02)00745-1.
^ Gbahou, F.; Rouleau, A.; Morisset, S.; Parmentier, R.; Crochet, S.; Lin, J. S.; Ligneau, X.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2003). „Protean agonism at histamine H3 receptors in vitro and in vivo”. Proceedings of the National Academy of Sciences of the United States of America. 100 (19): 11086—11091. PMC 196931 . PMID 12960366. doi:10.1073/pnas.1932276100 .
^ Baldi, E.; Bucherelli, C.; Schunack, W.; Cenni, G.; Blandina, P.; Passani, M. B. (2005). „The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat”. Neuropharmacology. 48 (2): 246—251. PMID 15695163. S2CID 24218659. doi:10.1016/j.neuropharm.2004.09.009. hdl:2158/220558.
^ Krueger, Kathleen M.; Witte, David G.; Ireland-Denny, Lynne; Miller, Thomas R.; Baranowski, John L.; Buckner, Steve; Milicic, Ivan; Esbenshade, Timothy A.; Hancock, Arthur A. (2005). „G Protein-Dependent Pharmacology of Histamine H₃ Receptor Ligands: Evidence for Heterogeneous Active State Receptor Conformations”. Journal of Pharmacology and Experimental Therapeutics. 314 (1): 271—281. PMID 15821027. S2CID 20470970. doi:10.1124/jpet.104.078865.
^ Arrang, J. M.; Morisset, S.; Gbahou, F. (2007). „Constitutive activity of the histamine H3 receptor”. Trends in Pharmacological Sciences. 28 (7): 350—357. PMID 17573125. doi:10.1016/j.tips.2007.05.002.
^ Baker, Jillian G. (2008). „Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells”. BMC Pharmacology. 8: 9. PMC 2430196 . PMID 18538007. doi:10.1186/1471-2210-8-9 .

Spoljašnje veze

[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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди

[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] Morisset, S.; Rouleau, A.; Ligneau, X.; Gbahou, F.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2000). „High constitutive activity of native H3 receptors regulates histamine neurons in brain”. Nature. 408 (6814): 860—864. PMID 11130725. S2CID 4391762. doi:10.1038/35048583.

[4] Fox, G. B.; Pan, J. B.; Esbenshade, T. A.; Bitner, R. S.; Nikkel, A. L.; Miller, T.; Kang, C. H.; Bennani, Y. L.; Black, L. A.; Faghih, R.; Hancock, A. A.; Decker, M. W. (2002). „Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model”. Pharmacology, Biochemistry, and Behavior. 72 (3): 741—750. PMID 12175472. S2CID 45861589. doi:10.1016/s0091-3057(02)00745-1.

[5] Gbahou, F.; Rouleau, A.; Morisset, S.; Parmentier, R.; Crochet, S.; Lin, J. S.; Ligneau, X.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2003). „Protean agonism at histamine H3 receptors in vitro and in vivo”. Proceedings of the National Academy of Sciences of the United States of America. 100 (19): 11086—11091. PMC 196931 . PMID 12960366. doi:10.1073/pnas.1932276100 .

[6] Baldi, E.; Bucherelli, C.; Schunack, W.; Cenni, G.; Blandina, P.; Passani, M. B. (2005). „The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat”. Neuropharmacology. 48 (2): 246—251. PMID 15695163. S2CID 24218659. doi:10.1016/j.neuropharm.2004.09.009. hdl:2158/220558.

[7] Krueger, Kathleen M.; Witte, David G.; Ireland-Denny, Lynne; Miller, Thomas R.; Baranowski, John L.; Buckner, Steve; Milicic, Ivan; Esbenshade, Timothy A.; Hancock, Arthur A. (2005). „G Protein-Dependent Pharmacology of Histamine H₃ Receptor Ligands: Evidence for Heterogeneous Active State Receptor Conformations”. Journal of Pharmacology and Experimental Therapeutics. 314 (1): 271—281. PMID 15821027. S2CID 20470970. doi:10.1124/jpet.104.078865.

[8] Arrang, J. M.; Morisset, S.; Gbahou, F. (2007). „Constitutive activity of the histamine H3 receptor”. Trends in Pharmacological Sciences. 28 (7): 350—357. PMID 17573125. doi:10.1016/j.tips.2007.05.002.

[9] Baker, Jillian G. (2008). „Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells”. BMC Pharmacology. 8: 9. PMC 2430196 . PMID 18538007. doi:10.1186/1471-2210-8-9 .

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