エホニジピン
- 関
- efonidipine hydrochloride
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/08/15 16:38:29」(JST)
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Efonidipine
|
Systematic (IUPAC) name |
2-(phenyl-(phenylmethyl)amino)ethyl 5-(5,5-dimethyl-2-oxo-1,3-dioxa-2λ5-phosphacyclohex-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylate
|
Clinical data |
Trade names |
Landel (ランデル) |
AHFS/Drugs.com |
International Drug Names |
Routes of
administration |
Oral |
Legal status |
Legal status |
|
Identifiers |
CAS Number |
111011-63-3 Y |
ATC code |
none |
PubChem |
CID 119171 |
ChemSpider |
106463 N |
UNII |
40ZTP2T37Q Y |
ChEMBL |
CHEMBL2074922 N |
Chemical data |
Formula |
C34H38N3O7P |
Molar mass |
631.65 g/mol |
SMILES
-
O=P1(OCC(CO1)(C)C)C/4=C(/N\C(=C(\C(=O)OCCN(c2ccccc2)Cc3ccccc3)C\4c5cccc([N+]([O-])=O)c5)C)C
|
InChI
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InChI=1S/C34H38N3O7P/c1-24-30(33(38)42-19-18-36(28-15-9-6-10-16-28)21-26-12-7-5-8-13-26)31(27-14-11-17-29(20-27)37(39)40)32(25(2)35-24)45(41)43-22-34(3,4)23-44-45/h5-17,20,31,35H,18-19,21-23H2,1-4H3 N
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Key:NSVFSAJIGAJDMR-UHFFFAOYSA-N N
|
NY (what is this?) (verify) |
Efonidipine (INN) is a dihydropyridine calcium channel blocker marketed by Shionogi & Co. of Japan. It was launched in 1995, under the brand name Landel (ランデル). The drug blocks both T-type and L-type calcium channels.[1]
It has also been studied in atherosclerosis[2] and acute renal failure.[3]
References
- ^ Tanaka H, Shigenobu K (2002). "Efonidipine hydrochloride: a dual blocker of L- and T-type Ca2+ channels". Cardiovasc. Drug Rev. 20 (1): 81–92. PMID 12070536.
- ^ Toyoda K, Kitahara M, Yamashita T, et al. (May 1994). "[Effect of efonidipine hydrochloride (NZ-105), a new dihydropyridine calcium antagonist, on the experimental atherosclerosis in cholesterol-fed rabbits]". Nippon Yakurigaku Zasshi (in Japanese). 103 (5): 231–9. PMID 8188119.
- ^ Shudo C, Masuda Y, Sugita H, Tanaka S, Tomita K (November 1994). "Effects of efonidipine hydrochloride (NZ-105), a new calcium antagonist, against acute renal failure in rats". Gen. Pharmacol. 25 (7): 1451–8. PMID 7896060.
- (Japanese) Landel ランデル (PDF) Shionogi & Co. April 2005.
English Journal
- Angiotensin II increases nerve-evoked contractions in mouse tail artery by a T-type Ca(2+) channel-dependent mechanism.
- Reardon TF1, Callaghan BP1, Brock JA2.
- European journal of pharmacology.Eur J Pharmacol.2015 Aug 15;761:11-8. doi: 10.1016/j.ejphar.2015.04.027. Epub 2015 Apr 28.
- Angiotensin II (Ang II) increases sympathetic nerve-evoked contractions of arterial vessels. Here the mechanisms underlying this effect were investigated in mouse tail artery. Isometrically mounted segments of mouse distal tail artery were used to investigate the effects of endothelium denudation, b
- PMID 25934568
- Determination of efonidipine in human plasma by LC-MS/MS for pharmacokinetic applications.
- Liu M1, Zhao H1, Tong Y1, Zhang D1, Wang X1, Zhang L1, Han J1, Liu H2.
- Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2014 Nov 11;103C:1-6. doi: 10.1016/j.jpba.2014.11.001. [Epub ahead of print]
- Efonidipine hydrochloride is a new generation dihydropyridine calcium channel blocker designed to inhibit both T-type and L-type calcium channels. For the first time, a simple and robust LC-MS/MS method was developed for the determination of efonidipine in human plasma over the range of 0.100-20.0ng
- PMID 25462114
- A molecular signature of tissues with pacemaker activity in the heart and upper urinary tract involves coexpressed hyperpolarization-activated cation and T-type Ca2+ channels.
- Hurtado R1, Bub G, Herzlinger D.
- FASEB journal : official publication of the Federation of American Societies for Experimental Biology.FASEB J.2014 Feb;28(2):730-9. doi: 10.1096/fj.13-237289. Epub 2013 Nov 4.
- Renal pacemakers set the origin and frequency of the smooth muscle contractions that propel wastes from the kidney to the bladder. Although congenital defects impairing this peristalsis are a leading cause of pediatric renal failure, the mechanisms underlying renal pacemaker activity remain unknown.
- PMID 24189942
Japanese Journal
- A crossover comparison of urinary albumin excretion as a new surrogate marker for cardiovascular disease among 4 types of calcium channel blockers
- Konoshita Tadashi,Makino Yasukazu,Kimura Tomoko,Fujii Miki,Morikawa Norihiro,Wakahara Shigeyuki,Arakawa Kenichiro,Inoki Isao,Nakamura Hiroyuki,Miyamori Isamu
- International Journal of Cardiology 166(2), 448-452, 2013-06-20
- … efonidipine, a T/L type; … 0.01): nifedipine CR 30.8 (17.3-81.1),* cilnidipine 33.9 (18.0-67.7),* efonidipine 51.0 (21.2-129.8), amlodipine 40.6 (18.7-94.7). … PAC at cilnidipine and efonidipine was significantly lower than that at amlodipine. …
- NAID 120005302291
- 重度な臨床症状を呈した心房細動の犬に対する塩酸エホニジピンの効果
- 福島 隆治,小宮 みぎわ
- 動物臨床医学 = Journal of Animal Clinical Research Foundation 22(2), 69-73, 2013-06-20
- 僧帽弁閉鎖不全症の薬物治療をしていた11歳の柴犬が,心房細動を発症した。来院時の血液化学検査で,グルコース, アラニンアミノトランスフェラーゼ, アスパラギン酸アミノトランスフェラーゼ, 血中尿素窒素 , クレアチニンの上昇,カリウムの低下が確認された。また,沈鬱状態であり,食欲廃絶など重度な臨床症状を呈していた.塩酸エホニジピンによる薬物療法を併用したところ,翌日には除細動され,300日を経過し …
- NAID 10031183010
- Effect of Efonidipine on TGF-β1-Induced Cardiac Fibrosis Through Smad2-Dependent Pathway in Rat Cardiac Fibroblasts
- Lei Bai,Hitomi Hirofumi,Mori Tatsuhiko [他],NAGA Yukiko,DEGUCHI Kazushi,MORI Hirohito,MASAKI Tsutomu,NAKANO Daisuke,KOBORI Hiroyuki,KITAURA Yasushi,NISHIYAMA Akira
- Journal of pharmacological sciences 117(2), 98-105, 2011-10-20
- … We examined effects of efonidipine, a dual T-type and L-type calcium channel blocker (CCB), on TGF-<I>β</I>1–induced fibrotic changes in neonatal rat cardiac fibroblast. … TGF-<I>β</I>1 (5 ng/mL) significantly increased Smad2 phosphorylation and [<SUP>3</SUP>H]-leucine incorporation, which were attenuated by pretreatment with efonidipine (10 <I>μ</I>M). …
- NAID 10029896161
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