Bifenilindanon A

Bifenilindanon A
(IUPAC) ime
	3’-(((2-ciklopentil-6,7-dimetil-1-okso-2,3-dihidro- 1H-inden-5-il)oksi)metil)bifenil-4-karboksilna kiselina
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	9868580
ChemSpider	8044271
ChEMBL	CHEMBL593013
Hemijski podaci
Formula	C30H30O4
Mol. masa	454,556 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C30H30O4/c1-18-19(2)28-25(15-26(29(28)31)22-7-3-4-8-22)16-27(18)34-17-20-6-5-9-24(14-20)21-10-12-23(13-11-21)30(32)33/h5-6,9-14,16,22,26H,3-4,7-8,15,17H2,1-2H3,(H,32,33) ; Key: KMKBEESNZAPKMP-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Bifenilindanon A (BINA, LS-193,571) je istraživački agens koji deluje kao potentni i selektivni pozitivni alosterni modulator za grupu II metabotropnih glutamatnih receptora podtipa mGluR2.

U životinjskim ispitivanjima je pokazano da ima anksiolitičko i antipsihotičko dejstvo,^[5] i da blokira dejstvo proizvedeno halucinogenim lekovima DOB. BINA i drugi selektivni mGluR2 pozitivni modulatori su potencijalna nova klasa lekova za tretman šizofrenije, i moguće je da oni imaju superiorna svojstva u odnosu na tradicionalne antipsihotike.^[6]

BINA umanjuje kokainsku samoadministraciju kod pacova, bez uticaja na apetit, i smatra se da je to svojstvo značajno poboljšanje u odnosu na mGluR_2/3 agonist LY-379,268^[7]

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
↑ Galici R, Jones CK, Hemstapat K et al. (2006). „Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice”. The Journal of Pharmacology and Experimental Therapeutics 318 (1): 173–85. DOI:10.1124/jpet.106.102046. PMID 16608916.
↑ Benneyworth MA, Xiang Z, Smith RL, Garcia EE, Conn PJ, Sanders-Bush E (2007). „A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis”. Molecular Pharmacology 72 (2): 477–84. DOI:10.1124/mol.107.035170. PMID 17526600.
↑ in, Xinchun; Semenova, Svetlana; Yang, Li; Ardecky, Robert; Sheffler, Douglas J; Dahl, Russell; Conn, P Jeffrey; Cosford, Nicholas DP et al. (2010). „The mGluR2 Positive Allosteric Modulator BINA Decreases Cocaine Self-Administration and Cue-Induced Cocaine-Seeking and Counteracts Cocaine-Induced Enhancement of Brain Reward Function in Rats”. Neuropsychopharmacology 35 (10): 2021–36. DOI:10.1038/npp.2010.82. PMC 2922422. PMID 20555310.

Vanjske veze

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[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] Galici R, Jones CK, Hemstapat K et al. (2006). „Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice”. The Journal of Pharmacology and Experimental Therapeutics 318 (1): 173–85. DOI:10.1124/jpet.106.102046. PMID 16608916.

[6] Benneyworth MA, Xiang Z, Smith RL, Garcia EE, Conn PJ, Sanders-Bush E (2007). „A selective positive allosteric modulator of metabotropic glutamate receptor subtype 2 blocks a hallucinogenic drug model of psychosis”. Molecular Pharmacology 72 (2): 477–84. DOI:10.1124/mol.107.035170. PMID 17526600.

[7] , Xinchun; Semenova, Svetlana; Yang, Li; Ardecky, Robert; Sheffler, Douglas J; Dahl, Russell; Conn, P Jeffrey; Cosford, Nicholas DP et al. (2010). „The mGluR2 Positive Allosteric Modulator BINA Decreases Cocaine Self-Administration and Cue-Induced Cocaine-Seeking and Counteracts Cocaine-Induced Enhancement of Brain Reward Function in Rats”. Neuropsychopharmacology 35 (10): 2021–36. DOI:10.1038/npp.2010.82. PMC 2922422. PMID 20555310.

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Bifenilindanon A

Reference

Vanjske veze

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