Search Results - "WHITEAKER, Kristi"
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Effects of Substitution on 9-(3-Bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a Dihydropyridine ATP-Sensitive Potassium Channel Opener
Published in Journal of medicinal chemistry (16-11-2006)“…Structure−activity relationships were investigated on the tricyclic dihydropyridine (DHP) KATP openers…”
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Structure-activity studies for a novel series of tricyclic dihydropyrimidines as KATP channel openers (KCOs)
Published in Bioorganic & medicinal chemistry letters (03-06-2002)Get full text
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Synthesis and Structure−Activity Relationships of a Novel Series of Tricyclic Dihydropyridine-Based KATP Openers That Potently Inhibit Bladder Contractions in Vitro
Published in Journal of medicinal chemistry (03-06-2004)“…Structure−activity relationships were investigated on a novel series of tricyclic dihydropyridine-containing KATP openers. This diverse group of analogues,…”
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4
Validation of FLIPR membrane potential dye for high throughput screening of potassium channel modulators
Published in Journal of biomolecular screening (01-10-2001)“…A fluorescence-based assay using the FLIPR Membrane Potential Assay Kit (FMP) was evaluated for functional characterization and high throughput screening (HTS)…”
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Structure−Activity Studies of Novel Cyanoguanidine ATP-Sensitive Potassium Channel Openers for the Treatment of Overactive Bladder
Published in Journal of medicinal chemistry (29-11-2007)“…A series of novel cyanoguanidine derivatives was designed and synthesized. Condensation of N-(1-benzotriazol-1-yl-2,2-dichloropropyl)-substituted benzamides…”
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Characterization of human urinary bladder KATP channels containing SUR2B splice variants expressed in L-cells
Published in European journal of pharmacology (12-01-2004)“…The molecular properties of the sulfonylurea receptor 2 (SUR2) subunits of K(ATP) channels expressed in urinary bladder were assessed by polymerase chain…”
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(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization
Published in The Journal of pharmacology and experimental therapeutics (01-10-2002)“…Alterations in the myogenic activity of the bladder smooth muscle are thought to serve as a basis for the involuntary detrusor contractions associated with the…”
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[125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding
Published in Molecular pharmacology (01-07-2003)“…Although ATP-sensitive K+ channels continue to be explored for their therapeutic potential, developments in high-affinity radioligands to investigate native…”
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10
Functional characterization of adenosine receptors and coupling to ATP-sensitive K+ channels in Guinea pig urinary bladder smooth muscle
Published in The Journal of pharmacology and experimental therapeutics (01-03-2002)“…Although multiple adenosine receptors have been identified, the subtype and underlying mechanisms involved in the relaxation response to adenosine in the…”
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Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder
Published in Bioorganic & medicinal chemistry letters (19-01-2004)“…Thiourea derivatives were identified as glyburide-reversible potassium channel openers through high-throughput screening. Based on these findings, a number of…”
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12
In vitro and in vivo characterization of a novel naphthylamide ATP‐sensitive K+ channel opener, A‐151892
Published in British journal of pharmacology (01-09-2004)“…Openers of ATP‐sensitive K+ channels are of interest in several therapeutic indications including overactive bladder and other lower urinary tract disorders…”
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13
Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK‐293 cells
Published in British journal of pharmacology (01-04-2000)“…The pharmacological properties of KATP channels generated by stable co‐expression of the sulphonylurea receptor SUR1 and the inwardly rectifying K+ channel…”
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Pharmacological characterization of a 1,4‐dihydropyridine analogue, 9‐(3,4‐dichlorophenyl)‐3,3,6,6‐tetramethyl‐3,4,6,7,9,10‐hexahydro‐1,8(2 H ,5 H )‐acridinedione (A‐184209) as a novel K ATP channel inhibitor
Published in British journal of pharmacology (01-01-2003)“…This study reports on the identification and characterization of a 1,4‐dihydropyridine analogue,…”
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15
Characterization of the ATP-sensitive potassium channels (KATP) expressed in guinea pig bladder smooth muscle cells
Published in The Journal of pharmacology and experimental therapeutics (01-04-1999)“…ATP-sensitive K+ (KATP) channels play an important role in the regulation of smooth muscle membrane potential. To investigate the properties of KATP channels…”
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Synthesis and Structure−Activity Relationships of a Novel Series of 2,3,5,6,7,9-Hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide KATP Channel Openers: Discovery of (−)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-Dioxide (A-278637), a Potent KATP Opener That Selectively Inhibits Spontaneous Bladder Contractions
Published in Journal of medicinal chemistry (03-06-2004)“…Structure−activity relationships were investigated on a novel series of sulfonyldihydropyridine-containing KATP openers. Ring sizes, absolute stereochemistry,…”
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Pharmacological and molecular characterization of ATP-sensitive K + channels in the TE671 human medulloblastoma cell line
Published in European journal of pharmacology (09-04-1999)“…ATP-sensitive K + (K ATP) channels in the human medulloblastoma TE671 cell line were characterized by membrane potential assays utilizing a potentiometric…”
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Fluorescence-based functional assay for sarcolemmal ATP-sensitive potassium channel activation in cultured neonatal rat ventricular myocytes
Published in Journal of pharmacological and toxicological methods (01-07-2001)“…Introduction: Activation of ATP-sensitive K + channels (K ATP) has been shown to induce ischemic preconditioning that serves as a protective mechanism in the…”
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Species comparison and pharmacological characterization of rat and human CB 2 cannabinoid receptors
Published in European journal of pharmacology (28-11-2004)“…Pharmacological effects of cannabinoid ligands are thought to be mediated through cannabinoid CB 1 and CB 2 receptor subtypes. Sequence analysis revealed that…”
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Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors
Published in European journal of pharmacology (28-11-2004)“…Pharmacological effects of cannabinoid ligands are thought to be mediated through cannabinoid CB1 and CB2 receptor subtypes. Sequence analysis revealed that…”
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