RIODIPINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H19F2NO5
Molecular Weight	367.344
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC(=O)C1=C(C)NC(C)=C(C1C2=CC=CC=C2OC(F)F)C(=O)OC

InChI

InChIKey=AZVFIZVKGSPGPK-UHFFFAOYSA-N

InChI=1S/C18H19F2NO5/c1-9-13(16(22)24-3)15(14(10(2)21-9)17(23)25-4)11-7-5-6-8-12(11)26-18(19)20/h5-8,15,18,21H,1-4H3

HIDE SMILES / InChI

Molecular Formula	C18H19F2NO5
Molecular Weight	367.344
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2517404 | http://infomeds.net/foridon.html | https://www.ncbi.nlm.nih.gov/pubmed/8377339

Riodipine is the blocker of calcium channels of L-type. Riodipine is indicated for the treatment of arterial hypertension, prevention of attacks of angina pectoris. Antiepileptic effect of riodipine was manifested by a decreased frequency and amplitude of interictal discharges and a less frequent appearance of ictal discharges. Riodipine increased latency to first convulsive episodes and delayed the development of generalized tonic-clonic seizures. Detected side effects are: arterial hypotension, tachycardia, hypostasis of shins, increase of a daily urine. Allergic reactions to the drug are possible. Nitrates, tricyclic antidepressants, and other anti-hypertensive drugs are able to potentiate of riodipine effects.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Heart phosphodiesterase 2 Target ID: CHEMBL2111408 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2165822	Inhibitor 8504
Voltage-gated L-type calcium channel 95 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2992533 \| http://infomeds.net/foridon.html	Blocker 555

Conditions

Condition	Modality	Targets	Highest Phase	Product
Angina pectoris 110 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3066967 https://www.ncbi.nlm.nih.gov/pubmed/8377339 http://lekmed.ru/lekarstva/antagonisty-kalciya/foridon.html	Preventing		Approved 8583	Foridon Approved Use Indicated for the treatment of arterial hypertension the I-II foot, hypertensive crisis, prevention of attacks of stenocardia against the increased arterial pressure, prevention of attacks of an angina of exertion. Launch Date 1987
Hypertension 575 Sources: http://lekmed.ru/lekarstva/antagonisty-kalciya/foridon.html https://www.ncbi.nlm.nih.gov/pubmed/18418924 https://www.ncbi.nlm.nih.gov/pubmed/2097399	Primary		Approved 8583	Foridon Approved Use Indicated for the treatment of arterial hypertension the I-II foot, hypertensive crisis, prevention of attacks of stenocardia against the increased arterial pressure, prevention of attacks of an angina of exertion. Launch Date 1987

C_max

Value	Dose	Co-administered	Analyte	Population
10.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4082636/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		RIODIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
80 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4082636/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		RIODIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/4082636/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		RIODIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C19 2057 CYP1A2 2153 CYP19A1 429	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 17.0	inconclusive [IC50 43.6486 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 54.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 102.0	no
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 4.0	yes [EC50 1.2589 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 4.0	yes [IC50 1.0964 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 5.0	yes [IC50 2.754 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 6.0	yes [IC50 4.3649 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 76 \| 78	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/68909#section=Biological-Test-Results Page: 101.0

PubMed

Title	Date	PubMed
[The prognosis of the antianginal effect of foridon compared to other antianginal preparations].	1993	8377339
[Anti-angina effect of foridon in patients with stable exertion-induced stenocardia].	1988-10	3066967
Effect of ryodipine on electromechanical parameters of heart and vessels, cAMP phosphodiesterase activity and swelling-contraction cycle of mitochondria.	1985	2992533
Effects of verapamil, diltiazem and ryosidine on the release of dopamine and acetylcholine in rabbit caudate nucleus slices.	1984-02	6144047

Patents

Sample Use Guides

In Vivo Use Guide

20-30 mg 3 times a day. The maximum daily dose - 150 mg. Course of treatment 2-3 weeks

Route of Administration: Oral

In Vitro Use Guide

Riodipine (10(-8) mol/l--10(-6) mol/l) suppresses contraction force and diminishes frequency of spontaneous contractions of the rabbit atria, and also displays antagonism to the effect of Ca2+ upon rabbit auricle contractions.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:18:27 GMT 2025` Edited by `admin` on `Mon Mar 31 18:18:27 GMT 2025`
Record UNII	W12VDB26LB
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FORIDON

Preferred Name

English

RIODIPINE

Official Name

English

RYODIPINE

Common Name

English

riodipine [INN]

Common Name

English

Riodipine [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C333