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Items: 1 to 20 of 102

1.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.

Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE.

Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057. Epub 2012 May 4.

PMID:
22626552
2.

Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.

Seko T, Kato M, Kohno H, Ono S, Hashimura K, Takimizu H, Nakai K, Maegawa H, Katsube N, Toda M.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2067-70.

PMID:
11514140
3.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.

Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4.

PMID:
23876987
4.

Structure-activity relationships of trimethoxybenzyl piperazine N-type calcium channel inhibitors.

Pajouhesh H, Feng ZP, Zhang L, Pajouhesh H, Jiang X, Hendricson A, Dong H, Tringham E, Ding Y, Vanderah TW, Porreca F, Belardetti F, Zamponi GW, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4153-8. doi: 10.1016/j.bmcl.2012.04.054. Epub 2012 Apr 19.

5.

Scaffold-based design and synthesis of potent N-type calcium channel blockers.

Zamponi GW, Feng ZP, Zhang L, Pajouhesh H, Ding Y, Belardetti F, Pajouhesh H, Dolphin D, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. doi: 10.1016/j.bmcl.2009.09.008. Epub 2009 Sep 11.

PMID:
19815411
6.

Discovery and evaluation of selective N-type calcium channel blockers: 6-unsubstituted-1,4-dihydropyridine-5-carboxylic acid derivatives.

Yamamoto T, Niwa S, Tokumasu M, Onishi T, Ohno S, Hagihara M, Koganei H, Fujita S, Takeda T, Saitou Y, Iwayama S, Takahara A, Iwata S, Shoji M.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3639-42. doi: 10.1016/j.bmcl.2012.04.051. Epub 2012 Apr 17.

PMID:
22560585
7.

Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers.

Knutsen LJ, Hobbs CJ, Earnshaw CG, Fiumana A, Gilbert J, Mellor SL, Radford F, Smith NJ, Birch PJ, Russell Burley J, Ward SD, James IF.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7. Epub 2006 Nov 6.

PMID:
17134896
8.

Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.

Pajouhesh H, Feng ZP, Ding Y, Zhang L, Pajouhesh H, Morrison JL, Belardetti F, Tringham E, Simonson E, Vanderah TW, Porreca F, Zamponi GW, Mitscher LA, Snutch TP.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83. doi: 10.1016/j.bmcl.2010.01.008. Epub 2010 Jan 7.

PMID:
20117000
9.

Analgesic effects of a substituted N-triazole oxindole (TROX-1), a state-dependent, voltage-gated calcium channel 2 blocker.

Abbadie C, McManus OB, Sun SY, Bugianesi RM, Dai G, Haedo RJ, Herrington JB, Kaczorowski GJ, Smith MM, Swensen AM, Warren VA, Williams B, Arneric SP, Eduljee C, Snutch TP, Tringham EW, Jochnowitz N, Liang A, Euan MacIntyre D, McGowan E, Mistry S, White VV, Hoyt SB, London C, Lyons KA, Bunting PB, Volksdorf S, Duffy JL.

J Pharmacol Exp Ther. 2010 Aug;334(2):545-55. doi: 10.1124/jpet.110.166363. Epub 2010 May 3.

10.

5beta-reduced neuroactive steroids are novel voltage-dependent blockers of T-type Ca2+ channels in rat sensory neurons in vitro and potent peripheral analgesics in vivo.

Todorovic SM, Pathirathna S, Brimelow BC, Jagodic MM, Ko SH, Jiang X, Nilsson KR, Zorumski CF, Covey DF, Jevtovic-Todorovic V.

Mol Pharmacol. 2004 Nov;66(5):1223-35. Epub 2004 Jul 27.

11.

A novel series of pyrazolylpiperidine N-type calcium channel blockers.

Subasinghe NL, Wall MJ, Winters MP, Qin N, Lubin ML, Finley MF, Brandt MR, Neeper MP, Schneider CR, Colburn RW, Flores CM, Sui Z.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4080-3. doi: 10.1016/j.bmcl.2012.04.075. Epub 2012 May 2.

PMID:
22608964
12.

Structure-activity study of L-amino acid-based N-type calcium channel blockers.

Seko T, Kato M, Kohno H, Ono S, Hashimura K, Takimizu H, Nakai K, Maegawa H, Katsube N, Toda M.

Bioorg Med Chem. 2003 Apr 17;11(8):1901-13.

PMID:
12659776
13.

Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.

Teodori E, Baldi E, Dei S, Gualtieri F, Romanelli MN, Scapecchi S, Bellucci C, Ghelardini C, Matucci R.

J Med Chem. 2004 Nov 18;47(24):6070-81.

PMID:
15537361
14.

L-Cysteine based N-type calcium channel blockers: structure-activity relationships of the C-terminal lipophilic moiety, and oral analgesic efficacy in rat pain models.

Seko T, Kato M, Kohno H, Ono S, Hashimura K, Takenobu Y, Takimizu H, Nakai K, Maegawa H, Katsube N, Toda M.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2267-9.

PMID:
12161113
15.

Selective N-type neuronal voltage-sensitive calcium channel blocker, SNX-111, produces spinal antinociception in rat models of acute, persistent and neuropathic pain.

Bowersox SS, Gadbois T, Singh T, Pettus M, Wang YX, Luther RR.

J Pharmacol Exp Ther. 1996 Dec;279(3):1243-9.

PMID:
8968347
16.

Synthesis and pharmacological evaluation of 2-(1-alkylpiperidin-4-yl)-n-[(1r)-1-(4-fluorophenyl)-2-methylpropyl]acetamide Derivatives as Novel Antihypertensive Agents.

Watanuki S, Matsuura K, Tomura Y, Okada M, Okazaki T, Ohta M, Tsukamoto S.

Chem Pharm Bull (Tokyo). 2012;60(2):223-34.

17.

Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels.

Yamamoto T, Niwa S, Ohno S, Onishi T, Matsueda H, Koganei H, Uneyama H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Shoji M.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):798-802. Epub 2005 Nov 23.

PMID:
16309909
18.

Discovery, structure-activity relationship study, and oral analgesic efficacy of cyproheptadine derivatives possessing N-type calcium channel inhibitory activity.

Yamamoto T, Niwa S, Iwayama S, Koganei H, Fujita S, Takeda T, Kito M, Ono Y, Saitou Y, Takahara A, Iwata S, Yamamoto H, Shoji M.

Bioorg Med Chem. 2006 Aug 1;14(15):5333-9. Epub 2006 Apr 17.

PMID:
16616501
19.

Discovery and SAR of a novel series of 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles as N-type calcium channel inhibitors.

Winters MP, Subasinghe N, Wall M, Beck E, Brandt MR, Finley MF, Liu Y, Lubin ML, Neeper MP, Qin N, Flores CM, Sui Z.

Bioorg Med Chem Lett. 2014 May 1;24(9):2057-61. doi: 10.1016/j.bmcl.2014.03.063. Epub 2014 Mar 28.

PMID:
24726803
20.

Neuronal N-type calcium channel blockers: a series of 4-piperidinylaniline analogs with analgesic activity.

Hu LY, Ryder TR, Rafferty MF, Siebers KM, Malone T, Chatterjee A, Feng MR, Lotarski SM, Rock DM, Stoehr SJ, Taylor CP, Weber ML, Miljanich GP, Millerman E, Szoke BG.

Drug Des Discov. 2000;17(1):85-93.

PMID:
10928451
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