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Chemical Compound Review

MaxiPost     (3S)-3-(5-chloro-2-methoxy- phenyl)-3...

Synonyms: Flindokalner, Maxipost (TN), CHEMBL266510, AG-J-69975, SureCN4877314, ...
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Disease relevance of BMS-204352


High impact information on BMS-204352

  • In rat models of permanent large-vessel stroke, BMS-204352 provided significant levels of cortical neuroprotection when administered two hours after the onset of occlusion, but had no effects on blood pressure or cerebral blood flow [4].
  • The maxi-K channel opener BMS-204352 attenuates regional cerebral edema and neurologic motor impairment after experimental brain injury [1].
  • Administration of 0.1 mg/kg BMS-204352 improved neurologic motor function at 1 and 2 weeks postinjury (P < 0.05) and reduced the extent of cerebral edema in the ipsilateral hippocampus, thalamus, and adjacent cortex (P < 0.05) [1].
  • In patch-clamp electrophysiology on cell lines expressing Kv7 channel subtypes, Maxipost (BMS-204352) exerted positive modulation of all neuronal Kv7 channels, whereas its R-enantiomer was a negative modulator [5].
  • At GABA(A) receptors (alpha1beta2gamma2s and alpha2beta2gamma2s) expressed in Xenopus oocytes, BMS-204352 was a negative modulator, and the R-enantiomer was a positive modulator [5].

Biological context of BMS-204352

  • Finally, a pronounced slowing of the deactivation kinetics was induced in particular by BMS-204352 [6].
  • The current study was designed to evaluate the dose proportionality and pharmacokinetics of BMS-204352 in rats [7].
  • In conclusion, the potential for a drug-drug interaction due to alterations in protein binding with BMS-204352 is unlikely [8].
  • As dose increased from 5 to 10 mg/kg, both BMS-204352 C(max) and AUC values increased in plasma and brain, somewhat greater in proportion to the increment in dose [9].
  • Bioavailability and extent of absorption data suggest evidence of first pass metabolism of BMS-204352 in the rat and dog [10].

Anatomical context of BMS-204352

  • After IA administration of radiolabeled BMS-204352 to rats, ca. 5.9 and 85% of radioactivity was recovered within 7 days in urine and feces, respectively; corresponding recoveries after PO dosing were 4.5 and 99.5%, respectively [10].
  • BMS-204352 crossed the blood-brain barrier with brain-to-plasma (B/P) ratios of approximately 7-11 [9].
  • In an open, parallel fashion, sixteen rats per gender received a single intraarterial dose of BMS-204352 as a 3-min infusion into the carotid artery at 0.4, 2.0, 5.0 and 10.0 mg/kg dose levels [7].
  • Rats (3 animals/group/time point) received a single intravenous dose of BMS-204352 as 5 mg/kg bolus, 5 mg/kg 30 min infusion, 5 mg/kg 60 min infusion, and 10 mg/kg bolus dose, into the jugular vein [9].
  • In an open, three-way crossover study, three beagle dogs received a single intravenous dose of BMS-204352 as a 6-min infusion into the femoral vein at 0.4, 0.9, and 2.0 mg/kg dose levels [11].

Associations of BMS-204352 with other chemical compounds

  • We have employed a cinchona alkaloid/Selectfluor-mediated enantioselective fluorination of the oxindole 2 to achieve the first enantioslective synthesis of BMS-204352 (MaxiPost, S-1), an effective opener of maxi-K channels [12].
  • KCNQ4 channel activation by BMS-204352 and retigabine [6].
  • The M-current blocker linopirdine inhibited the baseline current, as well as the BMS-204352-induced activation of the KCNQ4 channels [6].
  • 1,3-dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one (NS-1619) and (3S)-(+)-(5-chloro-2-methoxyphenyl-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one (BMS 204352) maxi-K channel openers significantly elevated CK2 activities that were reversible by iberiotoxin [13].

Gene context of BMS-204352

  • Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352 [14].
  • At 10 microM, BMS-204352 increased the steady state current at -30 mV by 12-fold, in contrast to the 2-fold increase observed for the other KCNQ channels [Schrøder et al., 2001] [14].
  • These results suggest that the novel maxi-K channel opener BMS-204352 may be selectively beneficial in the treatment of experimental TBI [1].
  • Two compounds, BMS-204352 and retigabine, presently in clinical trials for the treatment of stroke and epilepsy, respectively, have been proposed to exert their protective action via an activation of potassium channels [6].
  • Protein binding of BMS-204352 was determined in sera from several species, namely, rat, monkey, dog, and human [8].

Analytical, diagnostic and therapeutic context of BMS-204352


  1. The maxi-K channel opener BMS-204352 attenuates regional cerebral edema and neurologic motor impairment after experimental brain injury. Cheney, J.A., Weisser, J.D., Bareyre, F.M., Laurer, H.L., Saatman, K.E., Raghupathi, R., Gribkoff, V., Starrett , J.E., McIntosh, T.K. J. Cereb. Blood Flow Metab. (2001) [Pubmed]
  2. Amide N-glucuronidation of MaxiPost catalyzed by UDP-glucuronosyltransferase 2B7 in humans. Zhang, D., Zhao, W., Roongta, V.A., Mitroka, J.G., Klunk, L.J., Zhu, M. Drug Metab. Dispos. (2004) [Pubmed]
  3. Radiochemical synthesis and biodistribution of a novel maxi-K potassium channel opener. Kiesewetter, D.O., Jagoda, E.M., Starrett, J.E., Gribkoff, V.K., Hewawasam, P., Srinivas, N., Salazar, D., Eckelman, W.C. Nucl. Med. Biol. (2002) [Pubmed]
  4. Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels. Gribkoff, V.K., Starrett, J.E., Dworetzky, S.I., Hewawasam, P., Boissard, C.G., Cook, D.A., Frantz, S.W., Heman, K., Hibbard, J.R., Huston, K., Johnson, G., Krishnan, B.S., Kinney, G.G., Lombardo, L.A., Meanwell, N.A., Molinoff, P.B., Myers, R.A., Moon, S.L., Ortiz, A., Pajor, L., Pieschl, R.L., Post-Munson, D.J., Signor, L.J., Srinivas, N., Taber, M.T., Thalody, G., Trojnacki, J.T., Wiener, H., Yeleswaram, K., Yeola, S.W. Nat. Med. (2001) [Pubmed]
  5. Anxiolytic effects of Maxipost (BMS-204352) and retigabine via activation of neuronal Kv7 channels. Korsgaard, M.P., Hartz, B.P., Brown, W.D., Ahring, P.K., Strøbaek, D., Mirza, N.R. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  6. KCNQ4 channel activation by BMS-204352 and retigabine. Schrøder, R.L., Jespersen, T., Christophersen, P., Strøbaek, D., Jensen, B.S., Olesen, S.P. Neuropharmacology (2001) [Pubmed]
  7. Pharmacokinetics and dose proportionality of BMS-204352 after intraarterial administration to rats. Krishna, R., Shah, V.R., Srinivas, N. Biopharmaceutics & drug disposition. (2002) [Pubmed]
  8. In vitro protein binding studies with BMS-204352: lack of protein binding displacement interaction in human serum. Krishna, R., Yao, M., Kaczor, D., Vachharajani, N., Srinivas, N.R. Biopharmaceutics & drug disposition. (2001) [Pubmed]
  9. Effect of dose and input rate on the brain penetration of BMS-204352 following intravenous administration to rats. Krishna, R., Palme, H., Zeng, J., Srinivas, N. Biopharmaceutics & drug disposition. (2002) [Pubmed]
  10. Disposition of radiolabeled BMS-204352 in rats and dogs. Krishna, R., Yao, M., Srinivas, N.R., Shah, V., Pursley, J.M., Arnold, M., Vachharajani, N.N. Biopharmaceutics & drug disposition. (2002) [Pubmed]
  11. Pharmacokinetics and dose proportionality of BMS-204352 after intravenous administration to dogs. Krishna, R., Shah, V.R., Mantha, S., Vachharajani, N.N., Srinivas, N. Biopharmaceutics & drug disposition. (2002) [Pubmed]
  12. Enantioselective fluorination mediated by N-fluoroammonium salts of cinchona alkaloids: first enantioselective synthesis of BMS-204352 (MaxiPost). Shibata, N., Ishimaru, T., Suzuki, E., Kirk, K.L. J. Org. Chem. (2003) [Pubmed]
  13. Cilostazol enhances casein kinase 2 phosphorylation and suppresses tumor necrosis factor-alpha-induced increased phosphatase and tensin homolog deleted from chromosome 10 phosphorylation and apoptotic cell death in SK-N-SH cells. Kim, K.Y., Shin, H.K., Lee, J.H., Kim, C.D., Lee, W.S., Rhim, B.Y., Shin, Y.W., Hong, K.W. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  14. Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352. Dupuis, D.S., Schrøder, R.L., Jespersen, T., Christensen, J.K., Christophersen, P., Jensen, B.S., Olesen, S.P. Eur. J. Pharmacol. (2002) [Pubmed]
  15. The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels. Hewawasam, P., Gribkoff, V.K., Pendri, Y., Dworetzky, S.I., Meanwell, N.A., Martinez, E., Boissard, C.G., Post-Munson, D.J., Trojnacki, J.T., Yeleswaram, K., Pajor, L.M., Knipe, J., Gao, Q., Perrone, R., Starrett, J.E. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
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