NNC 55-0396

NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells. IC50 value: 6.8 nMTarget: Cav3.1 T-type channelNNC 55-0396 can be an essential tool in preventing human ovarian cancer cell proliferation as a result of its ability to inhibit the function of T-type Ca2+ channels. It is believed that NNC 55-0396 may functions by dissolving in or passing through the plasma membrane of cells.

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cardiovascular Disease

[1]. Arnulfo Quesadaa, Peter H. Bui, Gregg E. Homanics，et al. Comparison of mibefradil and derivative NNC 55-0396 effects on behavior, cytochrome P450 activity, and tremor in mouse models of essential tremor. European Journal of Pharmacology. 2011,659 (1): 30-36.

[2]. Timo Strünker, Normann Goodwin, Christoph Brenker, et al. The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm. Nature, 2011,471, 382-386.

[3]. Hideto Miwa, Jinsoo Koh, Yoshinori Kajimoto, et al. Effects of T-type calcium channel blockers on a parkinsonian tremor model in rats. Pharmacology Biochemistry and Behavior. 2011,97(4): 656-659.

[4]. Li M, Hansen JB, Huang L, et al. Towards selective antagonists of T-type calcium channels: design, characterization and potential applications of NNC 55-0396. Cardiovasc Drug Rev. 2005 Summer;23(2):173-96.

[5]. Huang L, Keyser BM, Tagmose TM, et al. NNC 55-0396 [(1S,2S)-2-(2-(N-[(3-benzimidazol-2-yl)propyl]-N-methylamino)ethyl)-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphtyl cyclopropanecarboxylate dihydrochloride]: a new selective inhibitor of T-type calcium channels. J Pharmacol Exp Ther. 2004 Apr;309(1):193-9.

Neomycin sulfate | Nifedipine | Acetylcholine chloride | Ionomycin | (S)-(-)-Bay K 8644 | Nimodipine | Mibefradil dihydrochloride | Levetiracetam | CDN 1163 | Dantrolene sodium | Thapsigargin | Flufenamic Acid | ABT 639 | Ranolazine dihydrochloride | Cromolyn (sodium)