"目錄號: HY-14656
Membrane Transporter/Ion Channel-
Diltiazem hydrochloride是鈣離子流入抑制劑（緩慢通道阻斷劑或鈣拮抗劑）。
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生物活性
Description
Diltiazem hydrochloride is aCa2+influx inhibitor (slow channel blocker or calcium antagonist).
In Vitro
Benzothiazepine Ca2+antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+channels[1]. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+influx stimulated by alpha adrenoceptor activation and high-K+depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K+and a low concentration of norepinephrine (NE)[2]. Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC50of 10-20 μM)[3].
In Vivo
Diltiazem produces a noncompetitive inhibition of Ca2+-induced contractions of depolarized rabbit aorta. Furthermore, there is a lack of parallelism between the smooth muscle effects of removal of [Ca2+]ex and of addition of diltiazem[2]. Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. The treatment of hyperthyroid rats with losartan diltiazem (4.7±0.7%; P < 0.001) significantly reduces the percentage of fibrosis areas in the left ventricle[4].? In conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreases the blood pressure and increases the heart rate after intravenous administration (0.03--1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduces the blood pressure of SHR[5].
Clinical Trial
Ventrus Biosciences, Inc-TKL Research, Inc.
CLARITHROMYCIN/DILTIAZEM [VA Drug Interaction]
September 2013
Phase 1
Mutual Pharmaceutical Company, Inc.
Healthy; Adult; Volunteer; Colchicine; Pharmacokinetics; Diltiazem; Cytochrome p450 3A4; P-glycoprotein
August 2008
Phase 1
CAMC Health System
Atrial Fibrillation-Atrial Flutter
December 2013
Phase 4
Brigham and Women's Hospital-National Heart, Lung, and Blood Institute (NHLBI)-Boston Children’s Hospital
Hypertrophic Cardiomyopathy
January 2006
Phase 2-Phase 3
Eisai Inc.
Healthy Subjects
October 2010
Phase 1
Ventrus Biosciences, Inc
Diltiazem Skin Sensitivity.
March 2013
Phase 1
Mohammad Ali Nazarinia-Shiraz University of Medical Sciences
Digital Ulcer of Scleroderma
June 2016
Phase 2
Antonios Likourezos-Maimonides Medical Center
Heart Rate and Rhythm Disorders
June 2009
Phase 4
Eisai Co., Ltd.-Eisai Inc.
Healthy Subjects
October 2016
Phase 1
Seoul National University Hospital
Atrial Fibrillation
August 2009
Phase 4
Ankara University
Coronary Artery Ectasia
June 2012
RaeAnn Hirschy-Kimberly Ackerbauer, PharmD, BCPS, BCCCP-Gary Peksa, PharmD, BCPS-Joshua DeMott, PharmD, BCPS, BCCCP-Paul O'Donnell, PharmD, BCPS, BCCCP-Rush University Medical Center
Atrial Fibrillation-Heart Failure
January 2010
Indiana University School of Medicine-Indiana University
Healthy
April 2006
Phase 4
S.L.A. Pharma AG
Chronic Anal Fissure
October 2010
Phase 3
Bristol-Myers Squibb-PRA Health Sciences
Atrial Fibrillation
September 2010
Phase 1
GlaxoSmithKline
Atherosclerosis
May 14, 2013
Phase 1
Actelion
Healthy Subjects
September 2015
Phase 1
University Hospital, Strasbourg, France
Ischaemia-reperfusion Injury
June 2002
Phase 3
Mahidol University
Hypertension-Craniotomy
February 2010
Phase 1-Phase 2
Ottawa Hospital Research Institute-Merck Sharp & Dohme Corp.
Hepatitis C-Hypertension
May 2012
Phase 1
Ventrus Biosciences, Inc
Skin Irritation
March 2013
Phase 1
Bristol-Myers Squibb
Thrombosis
July 2016
Phase 1
AstraZeneca
Drug Induced Constipation
May 2012
Phase 1
Ventrus Biosciences, Inc
Adult Subjects With Anal Fissures.
February 2013
Phase 1
University of South Florida
Idiopathic Pulmonary Arterial Hypertension-Primary Pulmonary Hypertension-Pulmonary Arterial Hypertension-Familial Primary Pulmonary Hypertension
July 2012
Kowa Research Institute, Inc.
Healthy
May 2011
Phase 4
AstraZeneca
Healthy Subjects
January 2016
Phase 1
Pennington Biomedical Research Center-Compellis Pharmaceuticals
Food Intake
October 2009
Phase 1
Bispebjerg Hospital-Sacomed ApS
Chronic Anal Fissure
September 2014
AstraZeneca
Healthy Volunteers-Pharmacologic Action
December 2013
Phase 1
Pfizer
Healthy Volunteers
July 2014
Phase 1
AstraZeneca
Pharmacokinetics
May 2010
Phase 1
King Saud University
Fissure in Ano
November 2014
Phase 4
Asker & Baerum Hospital-Vestre Viken Hospital Trust-Helse Sor-Ost
Atrial Fibrillation-Permanent Atrial Fibrillation
February 2016
Phase 4
Tehran University of Medical Sciences
Pain
October 2007
Phase 4
Food and Drug Administration (FDA)-Spaulding Clinical Research LLC
Drug-induced QT Prolongation-Pharmacokinetics-Pharmacodynamics
May 2014
Phase 1
Actelion
Healthy Subjects
May 2015
Phase 1
Fudan University
Acute Myocardial Infarction-Percutaneous Coronary Intervention
December 2006
Phase 4
Tehran University of Medical Sciences
Rapid Ventricular Response Atrial Fibrillation
February 2011
Phase 4
University Hospital, Lille-Ministry of Health, France
Flu
October 2017
Phase 2
Asker & Baerum Hospital
Atrial Fibrillation
April 2006
Phase 3
Chinese University of Hong Kong
Non-Cardiac Chest Pain
November 2004
Seoul National University Hospital
Stable Angina
September 2013
Phase 4
Republican Scientific Center for Emergency Medicine-Institute Of Cardiology & Internal Diseases, Kazakhstan
Metabolic Syndrome
January 2003
Phase 1-Phase 2
Eli Lilly and Company
Healthy Volunteers
November 2014
Phase 1
National Institute of Allergy and Infectious Diseases (NIAID)
HIV Infections-Cardiovascular Diseases-Hypertension
Phase 1
