Literature DB >> 12729644

Synthesis of water-soluble prodrugs of BMS-191011: a maxi-K channel opener targeted for post-stroke neuroprotection.

Piyasena Hewawasam1, Min Ding, Nathan Chen, Dalton King, Jay Knipe, Lorraine Pajor, Astrid Ortiz, Valentin K Gribkoff, John Starrett.   

Abstract

A variety of water-soluble prodrugs of BMS-191011 was synthesized and evaluated for solution state stability and rate of conversion to BMS-191011 in rat and human plasma. The deoxycarnitine ester prodrug (11c) was selected for clinical evaluation based on its superior chemical stability, crystallinity and cleavage to BMS-191011 in human plasma.

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Year:  2003        PMID： 12729644     DOI： 10.1016/s0960-894x(03)00296-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Role of calcium-activated potassium channels in acetylcholine-induced vasodilation of rat retinal arterioles in vivo.

Authors:  Asami Mori; Sachi Suzuki; Kenji Sakamoto; Tsutomu Nakahara; Kunio Ishii
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2010-10-27       Impact factor: 3.000

2.  Glioma big potassium channel expression in human cancers and possible T cell epitopes for their immunotherapy.

Authors:  Lisheng Ge; Neil T Hoa; Andrew N Cornforth; Daniela A Bota; Anthony Mai; Dong In Kim; Shiun-Kwei Chiou; Michelle J Hickey; Carol A Kruse; Martin R Jadus
Journal:  J Immunol       Date:  2012-07-27       Impact factor: 5.422

3.  Down-regulation of BK channel expression in the pilocarpine model of temporal lobe epilepsy.

Authors:  Luis F Pacheco Otalora; Eder F Hernandez; Massoud F Arshadmansab; Sebastian Francisco; Michael Willis; Boris Ermolinsky; Masoud Zarei; Hans-Guenther Knaus; Emilio R Garrido-Sanabria
Journal:  Brain Res       Date:  2008-01-18       Impact factor: 3.252

4.  Effective Activation of BKCa Channels by QO-40 (5-(Chloromethyl)-3-(Naphthalen-1-yl)-2-(Trifluoromethyl)Pyrazolo [1,5-a]pyrimidin-7(4H)-one), Known to Be an Opener of KCNQ2/Q3 Channels.

Authors:  Wei-Ting Chang; Sheng-Nan Wu
Journal:  Pharmaceuticals (Basel)       Date:  2021-04-21

5.  Assessment of Blood-Brain Barrier Permeability by Dynamic Contrast-Enhanced MRI in Transient Middle Cerebral Artery Occlusion Model after Localized Brain Cooling in Rats.

Authors:  Eun Soo Kim; Seung-Koo Lee; Mi Jung Kwon; Phil Hye Lee; Young-Su Ju; Dae Young Yoon; Hye Jeong Kim; Kwan Seop Lee
Journal:  Korean J Radiol       Date:  2016-08-23       Impact factor: 3.500

6.  High Efficacy by GAL-021: A Known Intravenous Peripheral Chemoreceptor Modulator that Suppresses BKCa-Channel Activity and Inhibits IK(M) or Ih.

Authors:  Te-Ling Lu; Zi-Han Gao; Shih-Wei Li; Sheng-Nan Wu
Journal:  Biomolecules       Date:  2020-01-25
  6 in total

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