Details
Stereochemistry | RACEMIC |
Molecular Formula | C33H34N4O6 |
Molecular Weight | 582.6463 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)OC(=O)C1=C(C)NC(N)=C(C1C2=CC(=CC=C2)[N+]([O-])=O)C(=O)OC3CN(C3)C(C4=CC=CC=C4)C5=CC=CC=C5
InChI
InChIKey=ZKFQEACEUNWPMT-UHFFFAOYSA-N
InChI=1S/C33H34N4O6/c1-20(2)42-32(38)27-21(3)35-31(34)29(28(27)24-15-10-16-25(17-24)37(40)41)33(39)43-26-18-36(19-26)30(22-11-6-4-7-12-22)23-13-8-5-9-14-23/h4-17,20,26,28,30,35H,18-19,34H2,1-3H3
Molecular Formula | C33H34N4O6 |
Molecular Weight | 582.6463 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/14636080Curator's Comment: description was created based on several sources, including
http://www.ube-ind.co.jp/english/news/2003/2003_03.htm
Sources: http://www.ncbi.nlm.nih.gov/pubmed/14636080
Curator's Comment: description was created based on several sources, including
http://www.ube-ind.co.jp/english/news/2003/2003_03.htm
Azelnidipine (INN; marketed under the brand name CalBlock) is a dihydropyridine calcium channel blocker. It is sold in Japan by Daiichi-Sankyo pharmaceuticals, Inc. Azelnidipine is a new dihydropyridine calcium channel antagonist with selectivity for both L-type and T-type Ca channels. It has recently been approved in Japan for the treatment of patients with hypertension. Results from clinical trials showed that long-term treatment with azelnidipine effectively controls blood pressure (BP) in a cohort of 95 patients with mild-to-moderate hypertension. The antihypertensive efficacy of azelnidipine in patients with mild-to-moderate hypertension was shown to be similar to that of amlodipine or nitrendipine in a randomised double-blind study. Azelnidipine and amlodipine controlled 24-hour BP to a similar extent. Azelnidipine is generally well tolerated. Vasodilator adverse events such as headache and hot facial flushes account for most of the adverse events. Its use is not associated with reflex tachycardia.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2095229 Sources: http://www.ncbi.nlm.nih.gov/pubmed/20881449 |
|||
Target ID: CHEMBL2362995 Sources: http://www.ncbi.nlm.nih.gov/pubmed/20881449 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Calblock Approved UseUnknown Launch Date1.04137923E12 |
Sample Use Guides
The normal dose for an adult is 8-16 mg of azelnidipine once daily, taken orally after breakfast. The maximum dosage is 16 mg/day. The initial dosage is to be 8 mg/day or less, to be adjusted as symptoms are monitored, up to 16 mg daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4102561/
azelnidipine inhibited rat aortic smooth muscle cell (RASMC) death in a concentration-dependent manner (10-100 nM) as well as inhibited JNK and p38 activation by mechanical stretch
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:16:15 UTC 2023
by
admin
on
Fri Dec 15 16:16:15 UTC 2023
|
Record UNII |
PV23P19YUG
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C333
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
272
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
DB09230
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
AZELNIDIPINE
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
C73023
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
PV23P19YUG
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
7109
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
65948
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
100000086081
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
m2170
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | Merck Index | ||
|
CHEMBL1275868
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
C061679
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
123524-52-7
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
SUB05650MIG
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY | |||
|
DTXSID3020120
Created by
admin on Fri Dec 15 16:16:16 UTC 2023 , Edited by admin on Fri Dec 15 16:16:16 UTC 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ENANTIOMER -> RACEMATE | |||
|
ENANTIOMER -> RACEMATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |