Comparative analysis of inactivated-state block of N-type (Ca v2.2) calcium channels

Inflammation Research

Volumn 60, Issue 7, 2011, Pages 683-693

  Vortherms, Timothy A ^a   Swensen, Andrew M ^a   Niforatos, Wende ^a   Limberis, James T ^a   Neelands, Torben R ^a   Janis, Richard S ^a   Thimmapaya, Rama ^a   Donnelly Roberts, Diana L ^a   Namovic, Marian T ^a   Zhang, Di ^a   Putman, C Brent ^a   Martin, Ruth L ^a   Surowy, Carol S ^a   Jarvis, Michael F ^a   Scott, Victoria E ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

Automated patch clamp electrophysiology; Cav2.2; Fluorometric imaging plate reader (FLIPR); N type calcium channels; QPatch HT; State dependent inhibition

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL CAV2.2; CALCIUM CHANNEL N TYPE; FLUNARIZINE; FLUSPIRILENE; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR2.1; MIBEFRADIL; NP 078585; NP 118809; OMEGA CONOTOXIN GVIA; OMEGA CONOTOXIN MVIIA; PIMOZIDE; POTASSIUM CHLORIDE; RECOMBINANT PROTEIN; TEODOREI 18; UNCLASSIFIED DRUG;

ARTICLE; AUTOMATION; CALCIUM TRANSPORT; CELL ASSAY; CELL MEMBRANE DEPOLARIZATION; CELL MEMBRANE POTENTIAL; CELL MEMBRANE STEADY POTENTIAL; CHANNEL GATING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; ELECTROPHYSIOLOGY; FLUORESCENCE ANALYSIS; FLUOROMETRIC IMAGING PLATE READER ASSAY; FLUOROMETRY; GENE OVEREXPRESSION; HUMAN; HUMAN CELL; HYPERPOLARIZATION; IC 50; NUCLEOTIDE SEQUENCE; PATCH CLAMP; QPATCH HT;

ANIMALS; CALCIUM; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, N-TYPE; CELL LINE; HUMANS; ION CHANNEL GATING; MEMBRANE POTENTIALS; PATCH-CLAMP TECHNIQUES;

EID: 80051670107     PISSN: 10233830     EISSN: 1420908X     Source Type: Journal    
DOI: 10.1007/s00011-011-0322-9     Document Type: Article

References (31)

1. Catterall WA, Scheuer T, Thomsen W, Rossie S. Structure and modulation of voltage-gated ion channels. Ann N Y Acad Sci. 1991;625:174-80.
2. Bao J, Li JJ, Perl ER. Differences in Ca2+ channels governing generation of miniature and evoked excitatory synaptic currents in spinal laminae I and II. J Neurosci. 1998;18:8740-50. (Pubitemid 28491740)
3. Heinke B, Balzer E, Sandkuhler J. Pre- and postsynaptic contributions of voltage-dependent Ca2+ channels to nociceptive transmission in rat spinal lamina I neurons. Eur J Neurosci. 2004;19:103-11. (Pubitemid 38122076)
4. Urban MO, Ren K, Sablad M, Park KT. Medullary N-type and P/Q-type calcium channels contribute to neuropathy-induced allodynia. Neuroreport. 2005;16:563-6. (Pubitemid 40586083)
5. Cizkova D, Marsala J, Lukacova N, Marsala M, Jergova S, Orendacova J, et al. Localization of N-type Ca2+ channels in the rat spinal cord following chronic constrictive nerve injury. Exp Brain Res. 2002;147:456-63. (Pubitemid 35440498)
6. Westenbroek RE, Hoskins L, Catterall WA. Localization of Ca2+ channel subtypes on rat spinal motor neurons, interneurons, and nerve terminals. J Neurosci. 1998;18:6319-30. (Pubitemid 28373237)
7. Yokoyama K, Kurihara T, Makita K, Tanabe T. Plastic change of N-type Ca channel expression after preconditioning is responsible for prostaglandin E2-induced long-lasting allodynia. Anesthesiology. 2003;99:1364-70. (Pubitemid 37475182)
8. Luo ZD, Chaplan SR, Higuera ES, Sorkin LS, Stauderman KA, Williams ME, et al. Upregulation of dorsal root ganglion (alpha)2(delta) calcium channel subunit and its correlation with allodynia in spinal nerve-injured rats. J Neurosci. 2001;21: 1868-75. (Pubitemid 32221370)
9. Newton RA, Bingham S, Case PC, Sanger GJ, Lawson SN. Dorsal root ganglion neurons show increased expression of the calcium channel alpha2delta-1 subunit following partial sciatic nerve injury. Brain Res Mol Brain Res. 2001;95:1-8. (Pubitemid 33000358)
10. Miljanich GP. Ziconotide: neuronal calcium channel blocker for treating severe chronic pain. Curr Med Chem. 2004;11:3029-40. (Pubitemid 39545572)
11. Malmberg AB, Yaksh TL. Effect of continuous intrathecal infusion of omega-conopeptides, N-type calcium-channel blockers, on behavior and antinociception in the formalin and hot-plate tests in rats. Pain. 1995;60:83-90.
12. Saegusa H, Kurihara T, Zong S, Kazuno A, Matsuda Y, Nonaka T, et al. Suppression of inflammatory and neuropathic pain symptoms in mice lacking the N-type Ca2+ channel. EMBO J. 2001;20:2349-56. (Pubitemid 32452852)
13. Kim C, Jun K, Lee T, Kim SS, McEnery MW, Chin H, et al. Altered nociceptive response in mice deficient in the alpha(1B) subunit of the voltage-dependent calcium channel. Mol Cell Neurosci. 2001;18:235-45. (Pubitemid 32846531)
14. Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, et al. Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker. J Pharmacol Exp Ther. 2010;334:545-55.
15. Feng ZP, Doering CJ, Winkfein RJ, Beedle AM, Spafford JD, Zamponi GW. Determinants of inhibition of transiently expressed voltage-gated calcium channels by omega-conotoxins GVIA and MVIIA. J Biol Chem. 2003;278:20171-8. (Pubitemid 36799212)
16. Bowersox SS, Singh T, Nadasdi L, Zukowska-Grojec Z, Valentino K, Hoffman BB. Cardiovascular effects of omegaconopeptides in conscious rats: mechanisms of action. J Cardiovasc Pharmacol. 1992;20:756-64.
17. Snutch TP. Targeting chronic and neuropathic pain: the N-type calcium channel comes of age. NeuroRx. 2005;2:662-70. (Pubitemid 41393273)
18. Winquist RJ, Pan JQ, Gribkoff VK. Use-dependent blockade of Cav2.2 voltage-gated calcium channels for neuropathic pain. Biochem Pharmacol. 2005;70:489-99. (Pubitemid 40978538)
19. Priest BT, Swensen AM, McManus OB. Automated electrophysiology in drug discovery. Curr Pharm Des. 2007;13:2325-37. (Pubitemid 47317026)
20. Dai G, Haedo RJ, Warren VA, Ratliff KS, Bugianesi RM, Rush A, et al. A high-throughput assay for evaluating state dependence and subtype selectivity of Cav2 calcium channel inhibitors. Assay Drug Dev Technol. 2008;6:195-212. (Pubitemid 351670382)
21. Lubin ML, Reitz TL, Todd MJ, Flores CM, Qin N, Xin H. A nonadherent cell-based HTS assay for N-type calcium channel using calcium 3 dye. Assay Drug Dev Technol. 2006;4:689-94. (Pubitemid 46218166)
22. Benjamin ER, Pruthi F, Olanrewaju S, Shan S, Hanway D, Liu X, et al. Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR. Biochem Pharmacol. 2006;72:770-82. (Pubitemid 44233545)
23. Lin Y, McDonough SI, Lipscombe D. Alternative splicing in the voltage-sensing region of N-type CaV2.2 channels modulates channel kinetics. J Neurophysiol. 2004;92:2820-30. (Pubitemid 40340493)
24. Pajouhesh H, Feng ZP, Ding Y, Zhang L, Pajouhesh H, Morrison JL, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010;20:1378-83.
25. Xiao W, Naso L, Bennett GJ. Experimental studies of potential analgesics for the treatment of chemotherapy-evoked painful peripheral neuropathies. Pain Med. 2008;9:505-17.
26. Snutch T, Feng Z, Doering C. A new class of N-type calcium channel blocker efficacious in animal models of chronic pain. Soc Neurosci Abstr. 2001; 27:465.1.
27. Margolskee RF, McHendry-Rinde B, Horn R. Panning transfected cells for electrophysiological studies. Biotechniques. 1993;15: 906-11. (Pubitemid 23333288)
28. Bean BP. Nitrendipine block of cardiac calcium channels: highaffinity binding to the inactivated state. Proc Natl Acad Sci USA. 1984;81:6388-92. (Pubitemid 15220843)
29. Xia M, Imredy JP, Koblan KS, Bennett P, Connolly TM. Statedependent inhibition of L-type calcium channels: cell-based assay in high-throughput format. Anal Biochem. 2004;327:74-81. (Pubitemid 38367985)
30. Belardetti F, Tringham E, Eduljee C, Jiang X, Dong H, Hendricson A, et al. A fluorescence-based high-throughput screening assay for the identification of T-type calcium channel blockers. Assay Drug Dev Technol. 2009;7:266-80.
31. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, et al. Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55:81-93.