MIBEFRADIL DIHYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C29H38FN3O3.2ClH
Molecular Weight	568.551
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.Cl.COCC(=O)O[C@]3(CCN(C)CCCC1=NC2=C(N1)C=CC=C2)CCC4=C(C=CC(F)=C4)[C@@H]3C(C)C

InChI

InChIKey=MTJLQTFHJIHXIX-GDUXWEAWSA-N

InChI=1S/C29H38FN3O3.2ClH/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);2*1H/t28-,29-;;/m0../s1

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C29H38FN3O3
Molecular Weight	495.6287
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7996461 | https://www.ncbi.nlm.nih.gov/pubmed/21256842 | https://www.fda.gov/ohrms/dockets/ac/98/briefingbook/1998-3454B1_03_WL32.pdf | https://www.drugbank.ca/drugs/DB01388 | https://www.ncbi.nlm.nih.gov/pubmed/26690767

Mibefradil is a calcium channel blocker, chemically unlike other compounds in the class, that was approved by the Food and Drug Administration (FDA), U.S.A. in June 1997 for the treatment of patients with hypertension and chronic stable angina. Shortly following its introduction, mibefradil was withdrawn from the market in the U.S.A. as well as in Europe. The reason for the voluntary withdrawal of the drug by Roche laboratories was claimed to be the result of new information about potentially harmful interactions with other drugs. Mibefradil is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 uM and 18.6 uM for T-type and L-type channels respectively. Mibefradil is a tetralol calcium channel blocking agent that inhibits the influx of calcium ions across both the T (low-voltage) and L (high-voltage) calcium channels of cardiac and vascular smooth muscle, with a greater selectivity for T channels. Vasodilation occurs in vascular smooth muscle, causing a decrease in peripheral vascular resistance and a resulting decrease in blood pressure. Mibefradil causes a slight increase in cardiac output during chronic dosing. Mibefradil slows sinus and atrioventricular (AV) node conduction, producing a slight reduction in heart rate and a slight increase in the PR interval. It has also been shown to slightly lengthen the corrected sinus node recovery time and AH interval and to raise the Wenckebach point. The mechanism by which mibefradil reduces angina is not known, but is thought to be attributed to a reduction in heart rate, total peripheral resistance (afterload), and the heart rate-systolic blood pressure product at any given level of exercise. The result of these effects is a decrease in cardiac workload and myocardial oxygen demand. Mibefradil has been repurposed from an abandoned antihypertensive to a targeted solid tumor treatment, and it has been rescued from drug-drug interactions by using short-term dose exposure. Tau is using the early success of mibefradil as a proof of concept to build a platform technology of Cav3 blockers for broad antitumor applications in combination with new targeted cancer therapies, well-established.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Voltage-gated T-type calcium channel alpha-1H subunit 7 Target ID: CHEMBL1859 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10991994	Blocker 555	32.0 nM [IC50]
Voltage-gated T-type calcium channel alpha-1G subunit 8 Target ID: CHEMBL4641 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10991994	Blocker 555	1.34 µM [IC50]
Voltage-gated L-type calcium channel alpha-1C subunit 44 Target ID: CHEMBL1940 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10991994	Blocker 555	202.0 nM [IC50]
Voltage-gated T-type calcium channel alpha-1I subunit 4 Target ID: CHEMBL5558 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18817368	Blocker 555	126.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Hypertension 575 Sources: http://adisinsight.springer.com/drugs/800000236 http://www.mims.com/malaysia/drug/info/mibefradil?mtype=generic	Primary	Withdrawn	Posicor Approved Use Treatment of hypertension, angina pectoris Launch Date 1997
Stable angina, chronic 2 Sources: http://adisinsight.springer.com/drugs/800000236 http://www.mims.com/malaysia/drug/info/mibefradil?mtype=generic	Primary	Withdrawn	Posicor Approved Use Treatment of hypertension, angina pectoris Launch Date 1997
Glioblastoma multiforme 30 Sources: https://clinicaltrials.gov/ct2/show/NCT02202993	Primary	Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
115 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
61 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
495 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
777 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
718 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
12574 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
9.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
35.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Analyte	Population
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9811158	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MIBEFRADIL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
87.5 mg 4 times / day steady, oral MTD Dose: 87.5 mg, 4 times / day Route: oral Route: steady Dose: 87.5 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/	unhealthy, 19.8 - 80.5 years Health Status: unhealthy Age Group: 19.8 - 80.5 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/	DLT: Alanine aminotransferase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Alanine aminotransferase increased (grade 3, 1 patient) Aspartate aminotransferase increased (grade 3, 1 patient) Sinus bradycardia (grade 1, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/

AEs

AE	Significance	Dose	Population
Sinus bradycardia	grade 1, 1 patient DLT, Disc. AE	87.5 mg 4 times / day steady, oral MTD Dose: 87.5 mg, 4 times / day Route: oral Route: steady Dose: 87.5 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/	unhealthy, 19.8 - 80.5 years Health Status: unhealthy Age Group: 19.8 - 80.5 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/
Alanine aminotransferase increased	grade 3, 1 patient DLT, Disc. AE	87.5 mg 4 times / day steady, oral MTD Dose: 87.5 mg, 4 times / day Route: oral Route: steady Dose: 87.5 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/	unhealthy, 19.8 - 80.5 years Health Status: unhealthy Age Group: 19.8 - 80.5 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/
Aspartate aminotransferase increased	grade 3, 1 patient DLT, Disc. AE	87.5 mg 4 times / day steady, oral MTD Dose: 87.5 mg, 4 times / day Route: oral Route: steady Dose: 87.5 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/	unhealthy, 19.8 - 80.5 years Health Status: unhealthy Age Group: 19.8 - 80.5 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/28371832/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
		inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1741 CYP3A 227 CYP2C8/9 42 CYP1A2 2153	P-gp 2052

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2C8/9 42	inhibitor 4027 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2014217/	no
CYP3A 317	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/28/8/895;https://pubmed.ncbi.nlm.nih.gov/14517191/	yes [IC50 0.8 uM]	yes (co-administration study) Comment: Coadministration of mibefradil increased the Cmax of midazolam 3-fold, the AUC 8- to 9-fold, and the t1/2 4-fold Sources: https://dmd.aspetjournals.org/content/28/8/895;https://pubmed.ncbi.nlm.nih.gov/14517191/
P-gp 1932	inhibitor 4027 Sources: https://dmd.aspetjournals.org/content/28/8/895	yes [IC50 1.6 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/9620098/	yes
CYP2D6 2546	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/9620098/	yes

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://dmd.aspetjournals.org/content/28/8/895	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubmed.ncbi.nlm.nih.gov/9765513/

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B2-0615	http://www.3bsc.com/index/pro_info.php?id=19971
AA Blocks	AA000CVK	https://www.aablocks.com/goods/Goods/detail?id=AA000CVK
Aaron Chemicals	AR000DNC	http://www.aaronchem.com/116666-63-8
abcr GmbH	AB450277	http://www.abcr.de/shop/en/AB450277
Achemtek	0102-014068	http://www.achemtek.com/116666-63-8
AHH Chemical co.,ltd	API-1585	http://www.ahhchemical.com/product/API-1585.html
AK Scientific, Inc. (AKSCI)	3848AH	http://www.aksci.com/item_detail.php?cat=3848AH
Ambeed	A186181	https://www.ambeed.com/products/116666-63-8.html
Ambinter	Amb22388695	http://www.ambinter.com/reference/22388695
AstaTech, Inc.	FD5011	http://www.astatechinc.com/CPSResult.php?CRNO=37150
Aurora Fine Chemicals LLC	A18.033.557	http://online.aurorafinechemicals.com/info?ID=A18.033.557
Aurora Fine Chemicals LLC	K16.774.691	http://online.aurorafinechemicals.com/info?ID=K16.774.691
BioChemPartner	BCP15607	http://www.biochempartner.com/116666-63-8-BCP15607
BioCrick	BCC1749	http://www.biocrick.com/Mibefradil-dihydrochloride-BCC1749.html
BioSynth	J-003469	https://www.biosynth.com/en/products/all-products/products/J-003469.html
BLD Pharm	BD140109	http://www.bldpharm.com/products/116666-63-8.html
Boerchem	BC238043	http://www.boerchem.com/?product_43014.html
Chem Scene	CS-1189	http://www.chemscene.com/116666-63-8.html
ChemMol	97900807	http://www.chemmol.com/chemmol/97900807.html
ChemShuttle	157254	http://www.chemshuttle.com/catalogsearch/result/?q=116666-63-8&cat=
Chemspace	CSSB00000053596	https://chem-space.com/CSSB00000053596
CSNpharm	CSN11439	https://www.csnpharm.com/products/mibefradil-dihydrochloride.html
DC Chemicals	DC7463	http://www.dcchemicals.com/product_show-Mibefradil_dihydrochloride.html
eNovation Chemicals	D372240	https://www.enovationchem.com/ProductDetails.asp?ProductID=D372240
eNovation Chemicals	D501894	https://www.enovationchem.com/ProductDetails.asp?ProductID=D501894
Excenen	EX-A2252	https://www.excenen.com/searchresultlist.php?id=116666-63-8
Lab Network	LN01327325	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01327325
Lan Pharmatech	LAN-B69433	http://www.lanpharmatech.com/product-9?_keywords=LAN-B69433
Matrix Scientific	207068	https://www.matrixscientific.com/207068.html
MedChem Express	HY-15553A	https://www.medchemexpress.com/Mibefradil-dihydrochloride.html
MolPort	MolPort-003-666-827	https://www.molport.com/shop/molecule-link/MolPort-003-666-827
MuseChem	I000599	https://www.musechem.com/product/I000599.html
Synblock Inc	SB17509	http://www.synblock.com/product/116666-63-8.html
Tocris	2198	https://www.tocris.com/products/mibefradil-dihydrochloride_2198
Vesino Industrial Co Ltd	VA11293	http://www.vsnchem.com/goto/product/22631/
Yuhao Chemical	CJ3053	http://www.chemyuhao.com/116644-53-2.html

PubMed

Title	Date	PubMed
T-type calcium channels in the regulation of afferent and efferent arterioles in rats.	2004-02	14583435
The sources and sequestration of Ca(2+) contributing to neuroeffector Ca(2+) transients in the mouse vas deferens.	2003-12-01	14500773
Cellular mechanism for mibefradil-induced vasodilation of renal microcirculation: studies in the isolated perfused hydronephrotic kidney.	2003-12	14639089
Effects of imatinib mesylate (STI571, Glivec) on the pharmacokinetics of simvastatin, a cytochrome p450 3A4 substrate, in patients with chronic myeloid leukaemia.	2003-11-17	14612892
The influence of calcium channel antagonists on isolated human distal radial arteries.	2003-11	14576511
Mechanism of active repolarization of inhibitory junction potential in murine colon.	2003-11	14561587
Thalamic control of visceral nociception mediated by T-type Ca2+ channels.	2003-10-03	14526084
Effect of mibefradil on CYP3A4 in vivo.	2003-10	14517191
Reversal of experimental neuropathic pain by T-type calcium channel blockers.	2003-09	14499432
Cav3.1 (alpha1G) T-type Ca2+ channels mediate vaso-occlusion of sickled erythrocytes in lung microcirculation.	2003-08-22	12869394
Mechanisms of lateral inhibition in the olfactory bulb: efficiency and modulation of spike-evoked calcium influx into granule cells.	2003-08-20	12930793
Spontaneous regenerative activity in mammalian retinal bipolar cells: roles of multiple subtypes of voltage-dependent Ca2+ channels.	2003-08-15	12916735
TGFbeta1 signaling via alphaVbeta6 integrin.	2003-08-07	12935295
Mibefradil: "Has the baby been thrown out with the bath water?".	2003-07	12851630
Effects of first and second generation calcium channel blockers on diastolic function of the failing hamster heart: relationship with coronary flow changes.	2003-07	12827040
A T-type calcium channel required for normal function of a mammalian mechanoreceptor.	2003-07	12808460
New target molecules in the drug control of blood pressure and circulation.	2003-03	12769645
Detection of proarrhythmia in the female rabbit heart: blinded validation.	2003-03	12716112
Loss of T-type calcium current in sensory neurons of rats with neuropathic pain.	2003-01	12502999
Regulation of ANP secretion by cardiac Na+/Ca2+ exchanger using a new controlled atrial model.	2003-01	12388435
Influence of R-type (Cav2.3) and t-type (Cav3.1-3.3) antagonists on nigral somatodendritic dopamine release measured by microdialysis.	2003	12895515
An ACTH- and ATP-regulated background K+ channel in adrenocortical cells is TREK-1.	2002-12-20	12368289
Selectivity of different calcium antagonists on T- and L-type calcium currents in guinea-pig ventricular myocytes.	2002-12	12457621
Different effects of mibefradil and amlodipine on coronary vessels and during beta-adrenergic stimulation in conscious dogs.	2002-12	12451323
Role of T-type calcium channels in myogenic tone of skeletal muscle resistance arteries.	2002-12	12388244
Effects of mibefradil on uterine contractility.	2002-11-22	12433596
Involvement of T-type calcium channels in the mechanism of action of 5-HT in rat glomerulosa cells: a novel signaling pathway for the 5-HT7 receptor.	2002-11	12530678
beta-Subunits: fine tuning of Ca(2+) channel block.	2002-11	12413805
Involvement of T-type calcium channels in excitatory junction potentials in rat resistance mesenteric arteries.	2002-11	12411411
Ca2+ entry via P/Q-type Ca2+ channels and the Na+/Ca2+ exchanger in rat and human neocortical synaptosomes.	2002-11	12382075
Calcium channel blockade limits transcriptional, translational and functional up-regulation of the cardiac calpain system after myocardial infarction.	2002-10-18	12393065
Mechanical and thermal antinociception in rats following systemic administration of mibefradil, a T-type calcium channel blocker.	2002-10-04	12270514
Blood pressure response to antihypertensive agents related to baseline blood pressure.	2002-10	12501904
Modulation by mibefradil of the histamine-induced Ca2+ entry in human aortic endothelial cells.	2002-10	12419882
T-channel-like pharmacological properties of high voltage-activated, nifedipine-insensitive Ca2+ currents in the rat terminal mesenteric artery.	2002-10	12359628
Differential involvement of Ca(2+) channels in survival and neurite outgrowth of cultured embryonic cockroach brain neurons.	2002-09	12205168
Evidence that action potential generation is not the exclusive determinant to trigger spontaneous myogenic contraction of guinea-pig urinary bladder smooth muscle.	2002-09	12193219
Local electric stimulation causes conducted calcium response in rat interlobular arteries.	2002-09	12167598
Neuronal T-type alpha 1H calcium channels induce neuritogenesis and expression of high-voltage-activated calcium channels in the NG108-15 cell line.	2002-08-15	12177183
Fractal pharmacokinetics of the drug mibefradil in the liver.	2002-08	12241211
The Ca(2+) channel antagonists mibefradil and pimozide inhibit cell growth via different cytotoxic mechanisms.	2002-08	12130671
Randomized comparison of T-type versus L-type calcium-channel blockade on exercise duration in stable angina: results of the Posicor Reduction of Ischemia During Exercise (PRIDE) trial.	2002-07	12094189
Selective L-type, T-type, and nonspecific calcium-channel blockers for stable angina pectoris.	2002-07	12094182
T-Type calcium channel alpha1G and alpha1H subunits in human retinoblastoma cells and their loss after differentiation.	2002-07	12091545
The role of T-type calcium channels in morphine analgesia, development of antinociceptive tolerance and dependence to morphine, and morphine abstinence syndrome.	2002-06-28	12072160
Voltage-dependent inward currents of interstitial cells of Cajal from murine colon and small intestine.	2002-06-15	12068041
A post-marketing observational study to assess the safety of mibefradil in the community in England.	2002-06	12078937
Impaired mechanisms of leukocyte adhesion in vitro by the calcium channel antagonist mibefradil.	2002-05	12374895
Impaired mechanisms of leukocyte adhesion in vitro by the calcium channel antagonist mibefradil.	2002-05	12374893
Emerging role of drug interaction studies in drug development: the good, the bad, and the unknown.	2001	12397858

Patents

Sample Use Guides

In Vivo Use Guide

50 mg once daily, increased if necessary.

Route of Administration: Oral

In Vitro Use Guide

Mibefradil (3 uM) inhibited the excitatory junction potentials (EJPs) in rat resistance mesenteric arteries by about 50%.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:12:30 GMT 2025` Edited by `admin` on `Mon Mar 31 18:12:30 GMT 2025`
Record UNII	842TUP3PQ8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MIBEFRADIL HYDROCHLORIDE

Preferred Name

English

MIBEFRADIL DIHYDROCHLORIDE

Official Name

English

POSICOR

Brand Name

English

(1S,2S)-[2-[[3-(2-Benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate, dihydrochloride

Common Name

English

MIBEFRADIL DIHYDROCHLORIDE [MI]

Common Name

English

MIBEFRADIL DIHYDROCHLORIDE [VANDF]

Common Name

English

ACETIC ACID, METHOXY-, 2-(2-((3-(1H-BENZIMIDAZOL-2-YL)PROPYL)METHYLAMINO)ETHYL)-6-FLUORO-1,2,3,4-TETRAHYDRO-1-(1-METHYLETHYL)-2-NAPHTHALENYL ESTER, DIHYDROCHLORIDE, (1S-CIS)-

Common Name

English

RO 40-5967/001

Code

English

Mibefradil hydrochloride [WHO-DD]

Common Name

English

MIBEFRADIL DIHYDROCHLORIDE [USAN]

Common Name

English

MIBEFRADIL HYDROCHLORIDE [MART.]

Common Name

English

RO-40-5967/001

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C333