Details
Stereochemistry | UNKNOWN |
Molecular Formula | C27H28N2O7 |
Molecular Weight | 492.5204 |
Optical Activity | ( + ) |
Additional Stereochemistry | Yes |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COCCOC(=O)C1=C(C)NC(C)=C(C1C2=CC(=CC=C2)[N+]([O-])=O)C(=O)OC\C=C\C3=CC=CC=C3
InChI
InChIKey=KJEBULYHNRNJTE-DHZHZOJOSA-N
InChI=1S/C27H28N2O7/c1-18-23(26(30)35-14-8-11-20-9-5-4-6-10-20)25(21-12-7-13-22(17-21)29(32)33)24(19(2)28-18)27(31)36-16-15-34-3/h4-13,17,25,28H,14-16H2,1-3H3/b11-8+
Molecular Formula | C27H28N2O7 |
Molecular Weight | 492.5204 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 1 |
Optical Activity | ( + / - ) |
DescriptionSources: http://adis.springer.com/drugs/800001274Curator's Comment: Description was created based on several sources, including
http://www.nevapress.com/cdr/full/17/4/341.pdf | https://www.ncbi.nlm.nih.gov/pubmed/19426250
Sources: http://adis.springer.com/drugs/800001274
Curator's Comment: Description was created based on several sources, including
http://www.nevapress.com/cdr/full/17/4/341.pdf | https://www.ncbi.nlm.nih.gov/pubmed/19426250
Cilnidipine (FRC-8653) is a dihydropyridine (DHP) type of calcium channel antagonist. The L-type Ca2+ channel blockade by cilnidipine affects predominantly vascular smooth muscle, thereby producing vasodilation of peripheral resistance vessels and coronary arteries. The blockade of N-type Ca2+ channels affects predominantly peripheral nerve endings of sympathetic neurons, thereby dilating blood vessels by lowering plasma catecholamine levels. Furthermore, renoprotective and neuroprotective effects as well as cardioprotective action of cilnidipine have been demonstrated in clinical practice or animal examinations. Cilnidipine was originated by Fuji & Rebio Pharmaceutical Co., Ltd. and developed jointly with Ajinomoto for the treatment of hypertension. Cilnidipine has been launched in Japan.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
4.77 null [pIC50] | |||
6.08 null [pIC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ATELEC Approved UseHypertension |
|||
Primary | Unknown Approved UseUnknown |
|||
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10841896 |
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Effect of cilnidipine, a novel dihydropyridine Ca++-channel antagonist, on N-type Ca++ channel in rat dorsal root ganglion neurons. | 1997 Mar |
|
Comparison of 24-hour blood pressure, heart rate, and autonomic nerve activity in hypertensive patients treated with cilnidipine or nifedipine retard. | 1998 Aug |
|
Comparison of the direct negative dromotropic effect of a new calcium channel blocker, cilnidipine, with that of nicardipine. | 2005 May |
|
Renoprotective effect of the L/N-type calcium channel antagonist cilnidipine on puromycin aminonucleoside-induced nephrosis in rats. | 2009 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.eapharma.co.jp/en/news/2013/1213.pdf
Normally once daily 5 to 10 mg of cilnidipine after breakfast orally for
adult patient. The dose can be increased or reduced according to the
age and symptoms. If the above dose is not effective enough, the dose
can be increased to 20 mg once daily. For severe hypertension, 10 to 20
mg of cilnidipine orally once daily after breakfast.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19650875
Cell viability of PC12 was not affected by low concentrations of cilnidipine up to 150 uM, but it was slightly decreased at 200 uM cilnidipine.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:18:07 GMT 2023
by
admin
on
Sat Dec 16 10:18:07 GMT 2023
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Record UNII |
S85436ZG85
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Record Status |
Validated (UNII)
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Record Version |
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118934-77-3
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132338-87-5
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Related Record | Type | Details | ||
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RACEMATE -> ENANTIOMER |