Chemistry:B115
From HandWiki
B115 (IUPAC name 1-methyl-4-[(E)-2-naphthalen-1-ylethenyl]-3,6-dihydro-2H-pyridine[1]) is an inhibitor of the enzyme choline acetyltransferase (ChAT).
In vivo activity
B115 inhibits human ChAT with an IC50 of 4.3 µM.[2] During in vivo testing, B115 has been found to partially protect against soman, a nerve agent, but it has been suggested that this may not be due to ChAT inhibition.[3][4]
References
- ↑ PubChem. "1-Methyl-4-(1-naphthylvinyl)-1,2,3,6-tetrahydropyridine hydrochloride" (in en). https://pubchem.ncbi.nlm.nih.gov/compound/6444143.
- ↑ "AID 52122 - Inhibition of choline acetyltransferase (CAT) enzyme - PubChem". https://pubchem.ncbi.nlm.nih.gov/bioassay/52122.
- ↑ Gray, A. P.; Platz, R. D.; Henderson, T. R.; Chang, T. C.; Takahashi, K.; Dretchen, K. L. (April 1, 1988). "Approaches to protection against nerve agent poisoning. (Naphthylvinyl)pyridine derivatives as potential antidotes". Journal of Medicinal Chemistry 31 (4): 807–814. doi:10.1021/jm00399a022. ISSN 0022-2623. PMID 3351860.
- ↑ Henderson, T. R.; Gray, A. P.; Platz, R. D.; Kellar, K. J.; Dretchen, K. L. (1991). "Inhibition of brain choline acetyltransferase in vivo: (E)-1-methyl-4-(1-naphthylvinyl)-1,2,3,6-tetrahydropyridine hydrochloride (B115), a depot form of a potent inhibitor". Toxicology and Applied Pharmacology 107 (2): 336–343. doi:10.1016/0041-008x(91)90213-x. ISSN 0041-008X. PMID 1994515. Bibcode: 1991ToxAP.107..336H.
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