NITRENDIPINE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H20N2O6
Molecular Weight	360.3612
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC(=O)C1=C(C)NC(C)=C(C1C2=CC=CC(=C2)[N+]([O-])=O)C(=O)OC

InChI

InChIKey=PVHUJELLJLJGLN-UHFFFAOYSA-N

InChI=1S/C18H20N2O6/c1-5-26-18(22)15-11(3)19-10(2)14(17(21)25-4)16(15)12-7-6-8-13(9-12)20(23)24/h6-9,16,19H,5H2,1-4H3

HIDE SMILES / InChI

Molecular Formula	C18H20N2O6
Molecular Weight	360.3612
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.hmdb.ca/metabolites/HMDB15187
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/68009568

Nitrendipine is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Intermediate conductance calcium-activated potassium channel protein 4 13 Target ID: CHEMBL4305 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10884437	Inhibitor 8504	0.9 µM [Kd]
Voltage-gated L-type calcium channel alpha-1C subunit 44 Target ID: CHEMBL2529 Sources: https://www.drugbank.ca/drugs/DB01054	Blocker 555	0.97 nM [IC50]
Voltage-gated L-type calcium channel alpha-1C subunit 44 Target ID: CHEMBL2830 Sources: https://www.drugbank.ca/drugs/DB01054	Blocker 555	1.08 nM [IC50]
Voltage-gated L-type calcium channel alpha-1D subunit 2 Target ID: CHEMBL4138 Sources: https://www.drugbank.ca/drugs/DB01054	Blocker 555	3.59 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: http://www.webhealthcentre.com/drugix/Nitrendipine_DI0096.aspx	Primary		Approved 8583	Nitrendipine Approved Use Nitrendipine is used to treat mild to moderate hypertension.

C_max

Value	Dose	Analyte	Population
8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3.31 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
18.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
33.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 μg/kg bw single, intravenous dose: 40 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.56 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 μg/kg bw single, intravenous dose: 40 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
45.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
26.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
38.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
71.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
48.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3179170/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
54.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3179170/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
29.6 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
65.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
27.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3435690/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
61.23 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3435690/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
11.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 μg/kg bw single, intravenous dose: 40 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
13.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 μg/kg bw single, intravenous dose: 40 μg/kg bw route of administration: Intravenous experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
11.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
12.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
13.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
14 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2713213/	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	DEHYDRONITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3179170/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
3.43 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3179170/	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED
10.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.56 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3435690/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.85 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3435690/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
1.7% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2054271/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:		NITRENDIPINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3435690/	2 mg single, intravenous dose: 2 mg route of administration: Intravenous experiment type: SINGLE co-administered:		NITRENDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
60 mg 1 times / day multiple, oral Higher than recommended Dose: 60 mg, 1 times / day Route: oral Route: multiple Dose: 60 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2744062/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2744062/	Sources: https://pubmed.ncbi.nlm.nih.gov/2744062/
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/	Other AEs: Dizziness, Angina pectori... Other AEs: Dizziness (grade 3, 1.2%) Angina pectori (grade 3, 2.4%) Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/	Disc. AE: Flushing, Palpitations... AEs leading to discontinuation/dose reduction: Flushing Palpitations Oedema Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/

AEs

AE	Significance	Dose	Population
Dizziness	grade 3, 1.2%	20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/
Angina pectori	grade 3, 2.4%	20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12923404/
Flushing	Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/
Oedema	Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/
Palpitations	Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2183868/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 substrate 1946	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 879 OATP1B3 961 MRP4 290 CYP1A2 2153 BSEP 550 CYP2E1 1060 CYP2C19 2057 MRP3 246 P-gp 1741 CYP19A1 429 OATP1B1 1079	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	no [IC50 >10 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNDc1NTM0In19	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNDc1NTM0In19	no [IC50 >10 uM]
MRP3 326	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1OTE4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTI4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	no [IC50 >133 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4507#section=BioAssay-Results Page: 622.0	no
MRP1 232	activator 342 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4507#section=BioAssay-Results Page: 96.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [IC50 0.3 uM]
BSEP 554	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw2MDIwIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [IC50 22.5 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [IC50 3 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw0MzAyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [IC50 68.2 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjk3NjY4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [Inhibition 10 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTIxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes [Inhibition 10 uM]
MRP2 625	activator 342 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1NzQ4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDQ3NTUzNCJ9fQ==	yes

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4507#section=BioAssay-Results Page: 29 \| 667	inconclusive
CYP3A4 1946	substrate 4014 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNDc1NTM0In19 \| https://pubmed.ncbi.nlm.nih.gov/1914375/	yes		yes (co-administration study) Comment: Cimetidine increased AUC by 1.54-fold and Cmax by 1.16-fold Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNDc1NTM0In19 \| https://pubmed.ncbi.nlm.nih.gov/1914375/

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMNDc1NTM0In19

PubMed

Title	Date	PubMed
Deoxynivalenol (Vomitoxin)-Induced Cholecystokinin and Glucagon-Like Peptide-1 Release in the STC-1 Enteroendocrine Cell Model Is Mediated by Calcium-Sensing Receptor and Transient Receptor Potential Ankyrin-1 Channel.	2015-06	25787141
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).	2013-12	24014644
FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1.	2013-09-05	23769903
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.	2010-12	20829430
Prevention of hypertensive crises in rats induced by acute and chronic norepinephrine excess.	2010-10	20665428
Differential roles of dihydropyridine calcium antagonist nifedipine, nitrendipine and amlodipine on gentamicin-induced renal tubular toxicity in rats.	2009-10-12	19698708
Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms.	2009-02	19029287
Synergism of hydrochlorothiazide and nitrendipine on reduction of blood pressure and blood pressure variability in spontaneously hypertensive rats.	2006-12	17112411
Characterization of the cloned human intermediate-conductance Ca2+-activated K+ channel.	1998-09	9730970
L-type calcium channels regulate gastrin release from human antral G cells.	1997-08	9277405
Evaluation of the efficacy and tolerability of nitrendipine in reducing both pressure and left ventricular mass in hypertensive type 2 diabetic patients.	1997-08	9250456
Influence of the angiotensin II type 1 receptor gene polymorphism on the effects of perindopril and nitrendipine on arterial stiffness in hypertensive individuals.	1996-12	8952600
Nitrendipine and enalapril improve albuminuria and glomerular filtration rate in non-insulin dependent diabetes.	1996-06	8743521
Antihypertensive effects of trandolapril and nitrendipine in the elderly: a controlled trial with special emphasis on time effect profiles.	1996-01	8642191
Effect of indomethacin on blood pressure control during treatment with nitrendipine.	1995-09	8535553
Delayed development of hypertension after short-term nitrendipine treatment.	1994-07	8021001
Doxazosin versus nitrendipine: a double-blind comparative study in patients adhering to a sodium-restricted diet.	1994-06	7947364
Combination treatment of enalapril with nitrendipine in rats with renovascular hypertension.	1994-01	8282322
Treatment of hypertensive emergency. Comparison of a new dosage form of the calcium antagonist nitrendipine with nifedipine capsules.	1994	8046120
Nocturnal hypotension and ACE inhibitors.	1993-06	8345498
Adverse effect of the calcium channel blocker nitrendipine on nephrosclerosis in rats with renovascular hypertension.	1992-08	1639466
Effects of nitrendipine, chlordiazepoxide, flumazenil and baclofen on the increased anxiety resulting from alcohol withdrawal.	1992-01	1557510
Acute and short-term effects of nitrendipine and diltiazem at rest and during exercise in hypertensive patients.	1991-11-01	1790542
Pharmacokinetics, bioavailability, metabolism and acute and chronic antihypertensive effects of nitrendipine in patients with chronic renal failure and moderate to severe hypertension.	1991-03	2054271
The place of isradipine in the treatment of hypertension.	1991-02	1827026
Regression of cardiovascular structural changes after long-term antihypertensive treatment with the calcium antagonist nitrendipine.	1991	1725798
Tolerance to nitrendipine in patients with arterial hypertension accompanying chronic renal failure.	1991	1723462
Microvascular effects of cocaine; interaction with nitrendipine and enalaprilat.	1991	1646895
Nitrendipine decreases benzodiazepine withdrawal seizures but not the development of benzodiazepine tolerance or withdrawal signs.	1990-11	1963805
Effects of nitrendipine and atenolol on blood pressure and intracellular sodium in hypertensive blacks.	1990-04	2338698
Systemic and regional hemodynamic interactions of perindopril and nitrendipine in the spontaneously hypertensive rat.	1990-04	1691399
Lacidipine: a calcium antagonist with potent and long-lasting antihypertensive effects in animal studies.	1990-04	1691398
Preclinical pharmacology of Ro 31-6930, a new potassium channel opener.	1990-02	1689412
[The effect of calcium antagonist nitrendipine on the morphological picture of experimentally-produced myocardial injuries in rats].	1990	2327189
Cocaine-induced small vessel spasm in isolated rat hearts.	1989-07	2774060
Nitrendipine versus hydrochlorothiazide in hypertensive patients over 70 years of age.	1989-03	2920503
Cosecretion of calcitonin and calcitonin gene-related peptide from cultured rat medullary thyroid C cells.	1989-02	2470235
Treatment of hypertension in the elderly with a new calcium channel blocking drug, nitrendipine.	1989-01	2642658
Calcium currents in embryonic and neonatal mammalian skeletal muscle.	1988-06	2458429
Effects of nitrendipine and cilazapril alone or in combination on hemodynamics and regional blood flows in conscious spontaneously hypertensive rats.	1988	2468061
Nitrendipine-stimulated release of prostacyclin-like substance in normal and atherosclerotic animals.	1987-04	3300663
Renal effects of 1,4-dihydropyridines in animal models of hypertension and renal failure.	1987	2441191
Relative potency of a beta-blocking and a calcium entry blocking agent as antihypertensive drugs in black patients.	1986	2869952
Predictors of blood pressure increases after withdrawal of antihypertensive therapy.	1985-12	2856766
The protective effect of nitrendipine on gentamicin acute renal failure in rats.	1985-08	3159593
Antihypertensive treatment using calcium antagonists in combination with captopril rather than diuretics.	1985	2580183
Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state.	1984-10	6093100
Clinical and systemic hemodynamic effects of nitrendipine.	1984-06	6734029
Systemic and regional hemodynamics in normotensive and spontaneously hypertensive rats after slow-channel calcium blocker nitrendipine.	1984	6733943
Mode of antihypertensive action of nitrendipine.	1984	6085384

Patents

Sample Use Guides

In Vivo Use Guide

Start with 5-20 mg once daily. May be increased to 40 mg in 1 or 2 doses. In hepatic disease reduce the dose to 5 to 10 mg daily.

Route of Administration: Oral

In Vitro Use Guide

At 1 and 10 uM, nitrendipine reduced peak Cav1.2a1 currents by 64+/-3% (n=4) and 81+/-1% (n=4), respectively, but at these same concentrations only inhibited Cav1.3a1 currents by 23+/-1% (n=8) and 53+/-2% (n=8), respectively.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 08:31:47 GMT 2025` Edited by `admin` on `Wed Apr 02 08:31:47 GMT 2025`
Record UNII	9B627AW319
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NITRENDIPINE

Official Name

English

BAYOTENSIN

Preferred Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, ETHYL METHYL ESTER

Common Name

English

NITRENDIPINE [USAN]

Common Name

English

NITRENDIPINE [EP MONOGRAPH]

Common Name

English

BAYPRESS

Brand Name

English

BAY-E-5009

Code

English

(±)-BAY-E-5009

Code

English

NSC-758466

Code

English

NITRENDIPINE [MI]

Common Name

English

NITRENDIPINE [MART.]

Common Name

English

(±)-ETHYL METHYL 1,4-DIHYDRO-2,6-DIMETHYL-4-(M-NITROPHENYL)-3,5-PYRIDINEDICARBOXYLATE

Systematic Name

English

NIDREL

Common Name

English

NITRENDIPINE [JAN]

Common Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, 3-ETHYL 5-METHYL ESTER

Common Name

English

NITREPIN

Common Name

English

(±)-NITRENDIPINE

Common Name

English

Nitrendipine [WHO-DD]

Common Name

English

DEITEN

Common Name

English

NITRENDIPINE [EP IMPURITY]

Common Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, ETHYL METHYL ESTER, (±)-

Common Name

English

nitrendipine [INN]

Common Name

English

BAY E 5009

Code

English

Classification Tree Code System Code

WHO-VATC

QC09BB06