C101, a novel 4-amino-piperidine derivative selectively blocks N-type calcium channels

European Journal of Pharmacology

Volumn 587, Issue 1-3, 2008, Pages 42-47

  Zhang, Shuzhuo ^a   Su, Ruibin ^a   Zhang, Cheng ^a   Liu, Xiaoyan ^a   Li, Jin ^a   Zheng, Jianquan ^a  

^a BEIJING INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY   (China)

Author keywords

Hippocampal neuron; N type Ca2+ channel; Pain; Xenopus oocyte

Indexed keywords

4 FLUROBENZYL [1 (4 DIETHYLAMINO) PIPERIDIN 4 YL] (2 ETHYLBUTYL) AMINE TRIHYDROCHLORIDE; C 101; CALCIUM CHANNEL L TYPE; CALCIUM CHANNEL N TYPE; CALCIUM CHANNEL P TYPE; CALCIUM CHANNEL Q TYPE; CALCIUM CHANNEL R TYPE; PIPERIDINE DERIVATIVE; POTASSIUM CHANNEL HERG; VOLTAGE GATED POTASSIUM CHANNEL; VOLTAGE GATED SODIUM CHANNEL;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DOSE RESPONSE; DRUG SELECTIVITY; HIPPOCAMPUS; IC 50; MEMBRANE POTENTIAL; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; STEADY STATE; XENOPUS;

ANIMALS; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, N-TYPE; CELLS, CULTURED; DNA, COMPLEMENTARY; ELECTROPHYSIOLOGY; ETHER-A-GO-GO POTASSIUM CHANNELS; HIPPOCAMPUS; HUMANS; OOCYTES; PIPERIDINES; RATS; SODIUM CHANNELS; XENOPUS;

EID: 44149116439     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2008.03.023     Document Type: Article

References (20)

1. Adams D.J., Smith A.B., Schroeder C.I., Yasuda T., and Lewis R.J. ω-Conotoxin CVID inhibits a pharmacologically distinct voltage-sensitive calcium channel associated with transmitter release from preganglionic nerve terminals. J. Biol. Chem. 278 (2003) 4057-4062
2. Banker G.A., and Cowan W.M. Further observations on hippocampus neurons in dispersed cell cultures. J. Comp. Neurol. 187 (1979) 469-493
3. Bell T.J., Thaler C., and Castiglioni A.J. Cell-specific alternative splicing increases calcium channel current density in the pain pathway. J. Neuron 41 (2004) 127-138
4. Bleakman D., Bowman D., Bath C.P., Brust P.F., Johnson E.C., Deal C.R., Miller R.J., Ellis S.B., Harpold M.M., and Hans M. Characteristics of a human N-type calcium channel expressed in HEK 293 cells. Neuropharmacology 34 (1995) 753-765
5. Canti C., Bogdanov Y., and Dolphin A.C. Interaction between G proteins and accessory subunits in the regulation of 1B calcium channels in Xenopus oocytes. J. Physiol. 527 (2000) 419-432
6. Dubel S.J., Starr T.V., Hell J., Ahlijanian M.K., Enyeart J.J., Catterall W.A., and Snutch T.P. Molecular cloning of the α-1 subunit of an ω-conotoxin-sensitive calcium channel. Proc. Natl. Acad. Sci. 89 (1992) 5058-5062
7. Field M.J., Cox P.J., Stott E., Melrose H., Offord J., Su T.Z., Bramwell S., Corradini L., England S., Winks J., Kinloch R.A., Hendrich J., Dolphin A.C., Webb T., and Williams D. Identification of the alpha2-delta-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin. Proc. Natl. Acad. Sci. U. S. A. 103 (2006) 17537-17542
8. 2+ channels. J. Physiol. 560 (2004) 351-363
9. 2+ channel blocker with oral activity for analgesia. Bioorg. Med. Chem. 8 (2000) 1203-1212
10. Llinas R., Steinberg I.Z., and Walton K. Relationship between presynaptic calcium current and postsynaptic potential in squid giant synapse. Biophys. J. 33 (1981) 323-351
11. McDonough S.I., Boland L.M., Mintz I.M., and Bean B.P. Interactions among toxins that inhibit N-type and P-type calcium channels. J. Gen. Physiol. 119 (2002) 313-328
12. McGivern J.G., and McDonough S.I. Voltage-gated calcium channels as targets for the treatment of chronic pain. Curr. Drug Targets CNS Neurol. Disord. 3 (2004) 457-478
13. Meir A., Ginsburg S., Butkevich A., Kachalsky S.G., Kaiserman I., Ahdut R., Demirgoren S., and Rahamimoff R. Ion channels in presynaptic nerve terminals and control of transmitter release. Physiol. Rev. 79 (1999) 1019-1088
14. Miljanich G.P. Ziconotide: neuronal calcium channel blocker for treating severe chronic pain. Curr. Med. Chem. 11 (2004) 3029-3040
15. Mould J., Yasuda T., Schroeder C.I., Beedle A.M., Doering C.J., Zamponi G.W., Adams D.J., and Lewis R.J. The alpha2delta auxiliary subunit reduces affinity of omega-conotoxins for recombinant N-type (Cav2.2) calcium channels. J. Biol. Chem. 279 (2004) 34705-34714
16. Pan J.Q., and Lipscombe D. Alternative splicing in the cytoplasmic II-III loop of the N type ca channel 1B subunit: functional differences are β subunit-specific. J. Neurosci. 20 (2000) 4769-4775
17. Sanguinetti M.C., and Tristani-Firouzi M. hERG potassium channels and cardiac arrhythmia. Nature 23 (2006) 463-469
18. Sutton K.G., Siok C., Stea A., Zamponi G.W., Heck S.D., Volkmann R.A., Ahlijanian M.K., and Snutch T.P. Inhibition of neuronal calcium channels by a novel peptide spider toxin, DW13.3. Mol. Pharmacol. 54 (1998) 407-418
19. Wakamori M., Mikala G., and Mori Y. Auxiliary subunits operate as a molecular switch in determining gating behaviour of the unitary N-type calcium channel current in Xenopus oocytes. J. Physiol. 517 (1999) 659-672
20. Zamponi G.W., and Snutch T.P. Decay of prepulse facilitation of N type calcium channels during G protein inhibition is consistent with binding of a single G beta subunit. Proc. Natl. Acad. Sci. 95 (1998) 4035-4039