A KCa1.1/BK channel activator
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BMS 204352

Item No. 29378

Technical Information
Formal Name
(3S)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-1,3-dihydro-6-(trifluoromethyl)-2H-indol-2-one
CAS Number
187523-35-9
Synonyms
  • (+)-BMS 204352
Molecular Formula
C16H10ClF4NO2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
λmax
211 nm
SMILES
FC(F)(F)C1=CC=C([C@](F)(C2=C(OC)C=CC(Cl)=C2)C(N3)=O)C3=C1
InChi Code
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
InChi Key
ULYONBAOIMCNEH-HNNXBMFYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BMS 204352 is an activator of large-conductance calcium-activated potassium (KCa1.1/BK) channels that increases KCa1.1 currents in X. laevis oocytes expressing human KCa1.1 in a calcium- and concentration-dependent manner.1 It decreases electrically induced population excitatory postsynaptic potentials (pEPSPs) in vitro in CA1 rat neurons and in anesthetized rats when administered at doses ranging from 0.005 to 1 mg/kg. BMS 204352 (0.001 and 0.3 mg/kg) reduces infarct volume in a rat model of ischemic stroke induced by middle cerebral artery occlusion (MCAO). It decreases edema in the ipsilateral hippocampus, thalamus, and adjacent cortex and time to find the platform in the Morris water maze in a rat model of fluid percussion-induced traumatic brain injury (TBI).2 BMS 204352 also reverses cortical hyperexcitability and reduces hyperactivity and grooming behaviors in the FmrI-/- mouse model of Fragile X syndrome.3 Formulations containing BMS 204352 have been used in the treatment of ischemic stroke.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gribkoff, V.K., Starrett, J.E., Jr., Dworetzky, S.I., et alTargeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels. Nat. Med. 7(4), 471-477 (2001).

    2. Cheney, J.A., Weisser, J.D., Bareyre, F.M., et alThe maxi-K channel opener BMS-204352 attenuates regional cerebral edema and neurologic motor impairment after experimental brain injury. J. Cereb. Blood Flow Metab. 21(4), 396-403 (2001).

    3. Carreno-Munoz, M.I., Martins, F., Medrano, M.C., et alPotential 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 (2018).