mibefradil

ミベフラジル

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/03/01 03:41:21」(JST)

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Mibefradil

Systematic (IUPAC) name
(1S,2S)-2-(2-((3-(1H-benzo[d]imidazol-2-yl)propyl) (methyl)amino)ethyl)-6-fluoro-1-isopropyl- 1,2,3,4-tetrahydronaphthalen-2-yl 2-methoxyacetate
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a607007
Routes of administration	Oral
Legal status	Withdrawn from market
Pharmacokinetic data
Bioavailability	70 %
Protein binding	> 99 %
Metabolism	Hepatic
Biological half-life	17-25 h
Identifiers
CAS Number	116644-53-2 Y
ATC code	C08CX01
PubChem	CID 60662
IUPHAR/BPS	2522
DrugBank	DB01388 N
ChemSpider	54673 N
UNII	27B90X776A N
KEGG	D08217 Y
ChEMBL	CHEMBL45816 N
Chemical data
Formula	C29H38FN3O3
Molar mass	495.63 g/mol
SMILES CC(C)[C@H]1C2=C(CC[C@@]1(CCN(C)CCCC3=NC4=CC=CC=C4N3)OC(=O)COC)C=C(C=C2)F
InChI InChI=1S/C29H38FN3O3/c1-20(2)28-23-12-11-22(30)18-21(23)13-14-29(28,36-27(34)19-35-4)15-17-33(3)16-7-10-26-31-24-8-5-6-9-25(24)32-26/h5-6,8-9,11-12,18,20,28H,7,10,13-17,19H2,1-4H3,(H,31,32)/t28-,29-/m0/s1 N Key:HBNPJJILLOYFJU-VMPREFPWSA-N N
Physical data
Melting point	128 °C (262 °F) (dihydrochloride salt)
NY (what is this?)  (verify)

Mibefradil (Posicor) is a drug for the treatment of hypertension and chronic angina pectoris. It belongs to a group known as calcium channel blockers.

The mechanism of action of mibefradil is characterized by the selective blockade of transient, low-voltage-activated (T-type) calcium channels over long-lasting, high-voltage-activated (L-type) calcium channels, which is probably responsible for many of its unique properties.

It is nonselective.

On June 8, 1998, Roche announced the voluntary withdrawal of the drug from the market, one year after approval by the FDA, due to the potential for drug interactions, some of them deadly, which may occur when it is taken together with some other medications.

Synthesis

Mibefradil synthesis: YU 22988  ZW 20087 

References

UpToDate Contents

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• 1. 不整脈治療におけるカルシウムチャネル遮断剤拮抗剤 calcium channel blockers in the treatment of cardiac arrhythmias

English Journal

• Functional importance of L- and p/q-type voltage-gated calcium channels in human renal vasculature.

• Hansen PB, Poulsen CB, Walter S, Marcussen N, Cribbs LL, Skott O, Jensen BL.SourceCardiovascular and Renal Research, University of Southern Denmark, Winslowparken 21, 3 DK-5000, Odense C, Denmark. pbhansen@health.sdu.dk.
• Hypertension.Hypertension.2011 Sep;58(3):464-70. Epub 2011 Jul 25.
• Calcium channel blockers are widely used for treatment of hypertension, because they decrease peripheral vascular resistance through inhibition of voltage-gated calcium channels. Animal studies of renal vasculature have shown expression of several types of calcium channels that are involved in kidne
• PMID 21788606

• On the origin of Rhythmic Calcium Transients in the ICC-MP of the Mouse Small Intestine.

• Lowie BJ, Wang XY, White EJ, Huizinga JD.Source1McMaster University.
• American journal of physiology. Gastrointestinal and liver physiology.Am J Physiol Gastrointest Liver Physiol.2011 Aug 11. [Epub ahead of print]
• Interstitial cells of Cajal associated with the myenteric plexus (ICC-MP) are pacemaker cells of the small intestine, producing the characteristic omnipresent electrical slow waves, which orchestrate peristaltic motor activity and are associated with rhythmic intracellular calcium oscillations in IC
• PMID 21836058

Japanese Journal

• Synthesis and pharmacological evaluation of 1-isopropyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel antihypertensive agents

• Watanuki Susumu,Matsuura Keisuke,Tomura Yuichi [他]
• Chemical and pharmaceutical bulletin 59(8), 1029-1037, 2011-08
• NAID 40018913899

• T-type Ca^<2+> channels contribute to IBMX/forskolin- and K^+-induced Ca^<2+> transients in porcine olfactory receptor neurons

• GAUTAM Shree Hari,OTSUGURO Ken-ichi,ITO Shigeo,SAITO Toshiyuki,HABARA Yoshiaki
• Neuroscience research : the official journal of the Japan Neuroscience Society 57(1), 129-139, 2007-01-01
• NAID 10021188420

Related Links

• Mibefradilとは - goo Wikipedia (ウィキペディア)

Mibefradil (Posicor) is a drug for the treatment of hypertension and chronic angina pectoris. It belongs to a group known as calcium channel blockers. It is nonselective. [1] On June 8, 1998, Roche announced the voluntary withdrawal ...

• DrugBank: Mibefradil

Mibefradil was withdrawn from the market in 1998 because of potentially harmful interactions with other drugs. For the treatment of angina and high blood pressure. Mibefradil is a tetralol calcium channel blocking agent that inhibits the ...

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