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
Identifikatori
ATC kod	none
PubChem	CID 9868580
ChemSpider	8044271
ChEMBL	CHEMBL593013
Hemijski podaci
Formula	C30H30O4
Molarna masa	454,556 g/mol
	SMILES c3cc(C(O)=O)ccc3-c(ccc4)cc4COc(c1C)cc(c(C2=O)c1C)CC2C5CCCC5; ;
	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 ;

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,^[1] 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.^[2]

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^[3]

Reference

^ Galici, R.; Jones, C. K.; 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. PMID 16608916. doi:10.1124/jpet.106.102046.
^ 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. PMID 17526600. doi:10.1124/mol.107.035170.
^ 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. PMC 2922422  . PMID 20555310. doi:10.1038/npp.2010.82.

Spoljašnje veze

[1] Galici, R.; Jones, C. K.; 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. PMID 16608916. doi:10.1124/jpet.106.102046.

[2] 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. PMID 17526600. doi:10.1124/mol.107.035170.

[3] , 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. PMC 2922422  . PMID 20555310. doi:10.1038/npp.2010.82.

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