Flindokalner

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Flindokalner
Clinical data
Other namesBMS-204352; BMS204352; MaxiPost
ATC code
  • None
Identifiers
  • (3S)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.438.134
Chemical and physical data
FormulaC16H10ClF4NO2
Molar mass359.70 g·mol−1
3D model (JSmol)
  • COC1=C(C=C(C=C1)Cl)[C@]2(C3=C(C=C(C=C3)C(F)(F)F)NC2=O)F
  • InChI=1S/C16H10ClF4NO2/c1-24-13-5-3-9(17)7-11(13)15(18)10-4-2-8(16(19,20)21)6-12(10)22-14(15)23/h2-7H,1H3,(H,22,23)/t15-/m0/s1
  • Key:ULYONBAOIMCNEH-HNNXBMFYSA-N

Flindokalner (BMS-204352, MaxiPost) is a drug which acts as an opener of BKCa large-conductance, calcium-activated potassium channels. It was unsuccessful in clinical trials as a potential treatment for stroke, but continues to be researched for other applications such as Fragile X syndrome.[1][2][3][4][5][6][7][8][9]

See also

References

  1. Gribkoff VK, Starrett JE, Dworetzky SI, Hewawasam P, Boissard CG, Cook DA, et al. (April 2001). "Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels". Nature Medicine. 7 (4): 471–477. doi:10.1038/86546. PMID 11283675.
  2. Jensen BS (2002). "BMS-204352: a potassium channel opener developed for the treatment of stroke". CNS Drug Reviews. 8 (4): 353–360. doi:10.1111/j.1527-3458.2002.tb00233.x. PMC 6741660. PMID 12481191.
  3. Malysz J, Buckner SA, Daza AV, Milicic I, Perez-Medrano A, Gopalakrishnan M (May 2004). "Functional characterization of large conductance calcium-activated K+ channel openers in bladder and vascular smooth muscle". Naunyn-Schmiedeberg's Archives of Pharmacology. 369 (5): 481–489. doi:10.1007/s00210-004-0920-y. PMID 15095032.
  4. Korsgaard MP, Hartz BP, Brown WD, Ahring PK, Strøbaek D, Mirza NR (July 2005). "Anxiolytic effects of Maxipost (BMS-204352) and retigabine via activation of neuronal Kv7 channels". The Journal of Pharmacology and Experimental Therapeutics. 314 (1): 282–292. doi:10.1124/jpet.105.083923. PMID 15814569.
  5. Laumonnier F, Roger S, Guérin P, Molinari F, M'rad R, Cahard D, et al. (September 2006). "Association of a functional deficit of the BKCa channel, a synaptic regulator of neuronal excitability, with autism and mental retardation". The American Journal of Psychiatry. 163 (9): 1622–1629. doi:10.1176/ajp.2006.163.9.1622. hdl:11380/1250915. PMID 16946189.
  6. Nardi A, Olesen SP (2008). "BK channel modulators: a comprehensive overview". Current Medicinal Chemistry. 15 (11): 1126–1146. doi:10.2174/092986708784221412. PMID 18473808.
  7. Hébert B, Pietropaolo S, Même S, Laudier B, Laugeray A, Doisne N, et al. (1 August 2014). "Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by a BKCa channel opener molecule". Orphanet Journal of Rare Diseases. 9 124. doi:10.1186/s13023-014-0124-6. PMC 4237919. PMID 25079250.
  8. Carreno-Munoz MI, Martins F, Medrano MC, Aloisi E, Pietropaolo S, Dechaud C, et al. (February 2018). "Potential Involvement of Impaired BKCa Channel Function in Sensory Defensiveness and Some Behavioral Disturbances Induced by Unfamiliar Environment in a Mouse Model of Fragile X Syndrome". Neuropsychopharmacology. 43 (3): 492–502. doi:10.1038/npp.2017.149. PMC 5770751. PMID 28722023.
  9. Bonnycastle K, Dobson KL, Blumrich EM, Gajbhiye A, Davenport EC, Pronot M, et al. (30 August 2023). "Reversal of cell, circuit and seizure phenotypes in a mouse model of DNM1 epileptic encephalopathy". Nature Communications. 14 (1) 5285. Bibcode:2023NatCo..14.5285B. doi:10.1038/s41467-023-41035-w. PMC 10468497. PMID 37648685.