NS19504: A novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions

Journal of Pharmacology and Experimental Therapeutics

Volumn 350, Issue 3, 2014, Pages 520-530

  Nausch, Bernhard ^b   Rode, Frederik ^a,d   Jørgensen, Susanne ^a,e   Nardi, Antonio ^a,f   Korsgaard, Mads P G ^a,g   Hougaard, Charlotte ^a,h   Bonev, Adrian D ^b   Brown, William D ^a,i   Dyhring, Tino ^a,h   Strøbæk, Dorte ^a,h   Olesen, Søren Peter ^a   Christophersen, Palle ^a,h   Grunnet, Morten ^a,j   Nelson, Mark T ^b,c   Rønn, Lars C B ^a,j  

^a NEUROSEARCH A S   (Denmark)

^b UNIVERSITY OF VERMONT   (United States)

^c UNIVERSITY OF MANCHESTER   (United Kingdom)

^d NOVO NORDISK A S   (Denmark)

^e Radiometer AS   (Denmark)

^f GRÜNENTHAL GMBH   (Germany)

^g Sophion Bioscience A/S   (Denmark)

^h Saniona Baltorpvej   (Denmark)

ⁱ PCOVERY   (Denmark)

^j H LUNDBECK A S   (Denmark)

more..

Author keywords

[No Author keywords available]

Indexed keywords

IBERIOTOXIN; LARGE CONDUCTANCE CALCIUM ACTIVATED POTASSIUM CHANNEL; NS 19504; POTASSIUM CHANNEL; POTASSIUM CHANNEL STIMULATING AGENT; POTASSIUM ION; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BLADDER FUNCTION; BLADDER MUSCLE; CONCENTRATION RESPONSE; EMBRYO; EVOKED MUSCLE RESPONSE; FLUORESCENCE IMAGING PLATE READER SCREENING; GUINEA PIG; HEK293 CELL LINE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; INTRACELLULAR RECORDING; MICTURITION; NONHUMAN; PATCH CLAMP TECHNIQUE; PRIORITY JOURNAL; PROTEIN EXPRESSION; SMOOTH MUSCLE CONTRACTION; SMOOTH MUSCLE RELAXATION; VALIDATION STUDY; WHOLE CELL;

ANIMALS; CALCIUM CHANNEL AGONISTS; FEMALE; GUINEA PIGS; HEK293 CELLS; HUMANS; LARGE-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM CHANNELS; MALE; MUSCLE CONTRACTION; MUSCLE RELAXATION; ORGAN CULTURE TECHNIQUES; URINARY BLADDER;

EID: 84904977328     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.113.212662     Document Type: Article

References (43)

1. + channel alpha- and beta-subunits in HEK293 cells. FEBS Lett 415:67-70.
2. Andersson KE (2010) Detrusor myocyte activity and afferent signaling. Neurourol Urodyn 29:97-106.
3. + channels. Mol Pharmacol 72:1033-1044.
4. +) channels (BK) protects the heart against ischemia-reperfusion injury. Pflugers Arch 457:979-988.
5. Brading AF (1997) A myogenic basis for the overactive bladder. Urology 50:57-67.
6. Buckner SA, Milicic I, Daza AV, Coghlan MJ, and Gopalakrishnan M (2002) Spontaneous phasic activity of the pig urinary bladder smooth muscle: characteristics and sensitivity to potassium channel modulators. Br J Pharmacol 135:639-648.
7. Chen M and Petkov GV (2009) Identification of large conductance calcium activated potassium channel accessory beta4 subunit in rat and mouse bladder smooth muscle. J Urol 182:374-381.
8. Christ GJ, Day NS, Day M, Santizo C, Zhao W, Sclafani T, Zinman J, Hsieh K, Venkateswarlu K, and Valcic M, et al. (2001) Bladder injection of "naked" hSlo/pcDNA3 ameliorates detrusor hyperactivity in obstructed rats in vivo. Am J Physiol Regul Integr Comp Physiol 281:R1699-R1709.
9. Darblade B, Behr-Roussel D, Oger S, Hieble JP, Lebret T, Gorny D, Benoit G, Alexandre L, and Giuliano F (2006) Effects of potassium channel modulators on human detrusor smooth muscle myogenic phasic contractile activity: potential therapeutic targets for overactive bladder. Urology 68:442-448.
10. Ghatta S, Nimmagadda D, Xu X, and O'Rourke ST (2006) Large-conductance, calcium-activated potassium channels: structural and functional implications. Pharmacol Ther 110:103-116.
11. Heppner TJ, Bonev AD, and Nelson MT (1997) Ca - activated K+ channels regulate action potential repolarization in urinary bladder smooth muscle. Am J Physiol 273:C110-C117.
12. 24+ transients evoked by nerve stimulation in rat urinary bladder smooth muscle. J Physiol 564:201-212.
13. Herrera GM, Etherton B, Nausch B, and Nelson MT (2005) Negative feedback regulation of nerve-mediated contractions by KCa channels in mouse urinary bladder smooth muscle. Am J Physiol Regul Integr Comp Physiol 289:R402-R409.
14. Holland M, Langton PD, Standen NB, and Boyle JP (1996) Effects of the BKCa channel activator, NS1619, on rat cerebral artery smooth muscle. Br J Pharmacol 117:119-129.
15. Hougaard C, Fraser MO, Chien C, Bookout A, Katofiasc M, Jensen BS, Rode F, Bitsch-Nørhave J, Teuber L, and Thor KB, et al. (2009) A positive modulator of K Ca 2 and K Ca 3 channels, 4,5-dichloro-1,3-diethyl-1,3-dihydro- benzoimidazol-2-one (NS4591), inhibits bladder afferent firing in vitro and bladder overactivity in vivo. J Pharmacol Exp Ther 328:28-39.
16. + channels regulate human detrusor smooth muscle function. Am J Physiol Cell Physiol 301:C903-C912.
17. Imai T, Okamoto T, Yamamoto Y, Tanaka H, Koike K, Shigenobu K, and Tanaka Y (2001) Effects of different types of K+ channel modulators on the spontaneous myogenic contraction of guinea-pig urinary bladder smooth muscle. Acta Physiol Scand 173:323-333.
18. Jørgensen S, Dyhring T, Brown DT, Strøbæk D, Christophersen P, and Demnitz J (2013) A high-throughput screening campaign for detection of Ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol 11:163-172.
19. Kobayashi H, Adachi-Akahane S, and Nagao T (2000) Involvement of BK(Ca) channels in the relaxation of detrusor muscle via beta-adrenoceptors. Eur J Pharmacol 404:231-238.
20. Layne JJ, Nausch B, Olesen SP, and Nelson MT (2010) The BK channel activation by NS11021 decreases excitability and contractility of bladder smooth muscle. Am J Physiol Regul Integr Comp Physiol 298:R378-R384.
21. + channels by high glucose. Circ Res 99:607-616.
22. + channel openers in bladder and vascular smooth muscle. Naunyn Schmiedebergs Arch Pharmacol 369:481-489.
23. + channel. J Biol Chem 279:36746-36752.
24. Mora TC and Suarez-Kurtz G (2005) Effects of NS1608, a BK(Ca) channel agonist, on the contractility of guinea-pig urinary bladder in vitro. Br J Pharmacol 144:636-641.
25. Nardi A and Olesen SP (2008) BK channel modulators: a comprehensive overview. Curr Med Chem 15:1126-1146.
26. Nausch B, Heppner TJ, and Nelson MT (2010) Nerve-released acetylcholine contracts urinary bladder smooth muscle by inducing action potentials independently of IP3-mediated calcium release. Am J Physiol Regul Integr Comp Physiol 299: R878-R888.
27. Obushak ND, Matiichuk VS, Vasylyshin RY, and Ostapyuk YV (2004) Heterocyclic syntheses on the basis of arylation products of unsaturated compounds. X. 3-Aryl-2-chloropropanals as reactants for the synthesis of 2-aminothiazole derivatives. Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) 40:383-389.
28. + channels in urinary bladder smooth muscle cells of the guinea pig. Jpn J Pharmacol 85:382-390.
29. Ohi Y, Yamamura H, Nagano N, Ohya S, Muraki K, Watanabe M, and Imaizumi Y (2001b) Local Ca(2+) transients and distribution of BK channels and ryanodine receptors in smooth muscle cells of guinea-pig vas deferens and urinary bladder. J Physiol 534:313-326.
30. + channels in mouse urinary bladder smooth muscle cells. Jpn J Pharmacol 84:97-100.
31. + channel regulates contractile activity of mouse urinary bladder smooth muscle. J Physiol 537:443-452.
32. + channels by beta-adrenoceptors in guinea pig urinary bladder smooth muscle. Am J Physiol Cell Physiol 288:C1255-C1263.
33. Ponte CG, McManus OB, Schmalhofer WA, Shen DM, Dai G, Stevenson A, Sur S, Shah T, Kiss L, and Shu M, et al. (2012) Selective, direct activation of high-conductance, calcium-activated potassium channels causes smooth muscle relaxation. Mol Pharmacol 81:567-577.
34. Roy S, Morayo Akande A, Large RJ, Webb TI, Camarasu C, Sergeant GP, McHale NG, Thornbury KD, and Hollywood MA (2012) Structure-activity relationships of a novel group of large-conductance Ca(2+)-activated K(+) (BK) channel modulators: the GoSlo-SR family. ChemMedChem 7:1763-1769.
35. Roy S, Large RJ, Akande AM, Kshatri A, Webb TI, Domene C, Sergeant GP, McHale NG, Thornbury KD, and Hollywood MA (2014) Development of GoSlo-SR-5-69, a potent activator of large conductance Ca2+-activated K+ (BK) channels. Eur J Med Chem 75:426-437.
36. Salkoff L, Butler A, Ferreira G, Santi C, and Wei A (2006) High-conductance potassium channels of the SLO family. Nat Rev Neurosci 7:921-931.
37. Tanaka M, Sasaki Y, Kimura Y, Fukui T, Hamada K, and Ukai Y (2003) A novel pyrrole derivative, NS-8, suppresses the rat micturition reflex by inhibiting afferent pelvic nerve activity. BJU Int 92:1031-1036.
38. Thorneloe KS, Meredith AL, Knorn AM, Aldrich RW, and Nelson MT (2005) Urodynamic properties and neurotransmitter dependence of urinary bladder contractility in the BK channel deletion model of overactive bladder. Am J Physiol Renal Physiol 289:F604-F610.
39. Uchida H, Shishido K, Nomiya M, and Yamaguchi O (2005) Involvement of cyclic AMP-dependent and -independent mechanisms in the relaxation of rat detrusor muscle via beta-adrenoceptors. Eur J Pharmacol 518:195-202.
40. Wager TT, Hou X, Verhoest PR, and Villalobos A (2010) Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties. ACS Chem Neurosci 1:435-449.
41. Weaver CD, Harden D, Dworetzky SI, Robertson B, and Knox RJ (2004) A thalliumsensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells. J Biomol Screen 9:671-677.
42. Werner ME, Knorn AM, Meredith AL, Aldrich RW, and Nelson MT (2007) Frequency encoding of cholinergic- and purinergic-mediated signaling to mouse urinary bladder smooth muscle: modulation by BK channels. Am J Physiol Regul Integr Comp Physiol 292:R616-R624.
43. Zhang JH, Chung TD, and Oldenburg KR (1999) A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 4:67-73.