Cinnarizine

Identification

Summary

Cinnarizine is a drug used for the management of labyrinthine disorder symptoms, including vertigo, tinnitus, nystagmus, nausea, and vomiting.

Generic Name

Cinnarizine

DrugBank Accession Number

DB00568

Background

First synthesized by Janssen Pharmaceuticals in 1955, cinnarizine is an anti-histaminic drug mainly used for the control of vestibular disorders and motion sickness. Cinnarizine is a specific calcium channel blocker that primarily works on the central vestibular system to interfere with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. Combination use of cinnarizine with other nootropics, such as piracetam resulted in enhanced effect of boosting brain oxygen supply.

Type

Small Molecule

Groups

Approved, Investigational

Structure

Similar Structures

Weight: Average: 368.524
Monoisotopic: 368.22524891
Chemical Formula: C₂₆H₂₈N₂

Synonyms

1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine
1-Benzhydryl-4-cinnamylpiperazin
1-Cinnamyl-4-(diphenylmethyl)piperazine
Cinarizina
Cinnarizine
Cinnarizinum

External IDs

5-23-01-00233
516 MD
516-MD
BRN 0626121
R 1575
R 516

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Pharmacology

Indication

For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Dose Form
Management of	Balance disorders		••••••••••••	•••••••• •••••••• • •••••• ••••••
Treatment of	Dizziness		••••••••••••	•••••••
Treatment of	Motion sickness		••••••••••••	•••••••
Used in combination to treat	Motion sickness	Combination Product in combination with: Domperidone (DB01184)	••••••••••••	••••••
Treatment of	Nausea		••••••••••••	•••••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.

Mechanism of action

Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.

Target	Actions	Organism
AHistamine H1 receptor	antagonist	Humans
AVoltage-dependent L-type calcium channel subunit alpha-1C	inhibitor	Humans
AVoltage-dependent L-type calcium channel subunit alpha-1D	inhibitor	Humans
AVoltage-dependent L-type calcium channel subunit alpha-1F	inhibitor	Humans
AVoltage-dependent L-type calcium channel subunit alpha-1S	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1G	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1H	inhibitor	Humans
AVoltage-dependent T-type calcium channel subunit alpha-1I	inhibitor	Humans
NDopamine D2 receptor	other/unknown	Humans
UD(1) dopamine receptor	binder	Humans
UMuscarinic acetylcholine receptor	binder	Humans

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

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Cinnarizine

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects

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Toxicity

Not Available

Pathways

Pathway	Category
Cinnarizine H1-Antihistamine Action	Drug action

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Abametapir	The serum concentration of Cinnarizine can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Cinnarizine can be increased when combined with Abatacept.
Abiraterone	The serum concentration of Cinnarizine can be increased when it is combined with Abiraterone.
Abrocitinib	The metabolism of Abrocitinib can be decreased when combined with Cinnarizine.
Acarbose	The risk or severity of hypoglycemia can be increased when Cinnarizine is combined with Acarbose.

Food Interactions

Not Available

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Cinnarizine hydrochloride	5AKM4OA6VO	25332-14-3	LYXJDKBTSDYXQV-RSGUCCNWSA-N

International/Other Brands

Cinazyn (Italchimici) / Cinnageron (Streuli Pharma) / Folcodal (Ivax) / Sepan (Janssen-Cilag) / Stugeron (Janssen) / Stugeron Forte (Janssen) / Toliman (Scharper)

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
AXCEL CINNARIZINE TABLETS 25 mg	Tablet	25 mg	Oral	KOTRA PHARMA MARKETING	1999-05-17	Not applicable
CELENID TABLET 25 mg	Tablet	25 mg	Oral	MEDISPEC RENAISSANCE PTE. LTD.	1991-08-21	Not applicable
CINNA TABLET 25 mg	Tablet	25 mg	Oral	YUNG SHIN PHARMACEUTICAL (SINGAPORE) PTE LTD	1995-12-16	Not applicable
CINNAR TABLET 25 mg	Tablet	25 mg	Oral	ATLANTIC PHARMACEUTICAL (S) PTE LTD	1997-06-19	Not applicable
CINNARON 25 TABLET 25 mg	Tablet	25 mg	Oral	GOLDPLUS UNIVERSAL PTE LTD	1989-05-22	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Arlevert 20 mg/40 mg Tabletten	Cinnarizine (20 mg) + Dimenhydrinate (40 mg)	Tablet	Oral	Hennig Arzneimittel Gmb H & Co Kg	2007-09-06	Not applicable

Chemical Identifiers

UNII: 3DI2E1X18L
CAS number: 298-57-7
InChI Key: DERZBLKQOCDDDZ-JLHYYAGUSA-N
InChI: InChI=1S/C26H28N2/c1-4-11-23(12-5-1)13-10-18-27-19-21-28(22-20-27)26(24-14-6-2-7-15-24)25-16-8-3-9-17-25/h1-17,26H,18-22H2/b13-10+
IUPAC Name: 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
SMILES: C(\C=C\C1=CC=CC=C1)N1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1

References

Synthesis Reference

Janssen, P.A.J.; U.S. Patent 2,882,271; April 14, 1959; assigned to Laboratoria Pharmaceutica Dr. C. Janssen, Belgium.

General References

Not Available

External Links

KEGG Drug: D01295
PubChem Compound: 2761
PubChem Substance: 46506769
ChemSpider: 1264793
BindingDB: 50017657
RxNav: 2549
ChEBI: 31403
ChEMBL: CHEMBL43064
ZINC: ZINC000019632891
Therapeutic Targets Database: DAP000325
PharmGKB: PA164749342
PDBe Ligand: N90
Wikipedia: Cinnarizine

PDB Entries

7uhf

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Methamphetamine-induced Psychosis	1
Not Available	Active Not Recruiting	Treatment	Endocrine hypertension / Primary Aldosteronism	1
Not Available	Unknown Status	Prevention	Simulator Sickness	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Tablet	Oral
Tablet	Oral	75.00 mg
Capsule, liquid filled	Oral	75 mg
Tablet	Oral	75.0 mg
Tablet, film coated	Oral
Tablet	Oral
Tablet	Oral	75 mg
Capsule		100 MG
Capsule		75 MG
Solution / drops	Oral	75 MG/ML
Suspension	Oral	75 mg
Capsule
Solution / drops	Oral
Tablet	Oral	75.000 mg
Capsule		25 mg
Tablet	Oral	25 mg
Tablet, coated	Oral	25 mg

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	750 mg/L (at 25 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	5.77	BIOBYTE (1995)

Predicted Properties

Property	Value	Source
logP	5.88	Chemaxon
pKa (Strongest Basic)	8.1	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	2	Chemaxon
Hydrogen Donor Count	0	Chemaxon
Polar Surface Area	6.48 Å²	Chemaxon
Rotatable Bond Count	6	Chemaxon
Refractivity	119.86 m³·mol^-1	Chemaxon
Polarizability	43.97 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	Yes	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9506
Blood Brain Barrier	+	0.977
Caco-2 permeable	+	0.6409
P-glycoprotein substrate	Substrate	0.7107
P-glycoprotein inhibitor I	Inhibitor	0.7461
P-glycoprotein inhibitor II	Non-inhibitor	0.8398
Renal organic cation transporter	Inhibitor	0.7902
CYP450 2C9 substrate	Non-substrate	0.8549
CYP450 2D6 substrate	Substrate	0.8919
CYP450 3A4 substrate	Non-substrate	0.7558
CYP450 1A2 substrate	Inhibitor	0.7732
CYP450 2C9 inhibitor	Non-inhibitor	0.9488
CYP450 2D6 inhibitor	Inhibitor	0.8931
CYP450 2C19 inhibitor	Non-inhibitor	0.9026
CYP450 3A4 inhibitor	Non-inhibitor	0.9346
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.5
Ames test	Non AMES toxic	0.9279
Carcinogenicity	Non-carcinogens	0.9496
Biodegradation	Not ready biodegradable	0.9968
Rat acute toxicity	2.0618 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Strong inhibitor	0.5724
hERG inhibition (predictor II)	Non-inhibitor	0.524

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014i-0109000000-6aafd7aead713e954b51
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014i-0029000000-a8411e2cfb4c21265d14
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014i-0906000000-ef5571072f8d2c31a967
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014i-0009000000-961c386872609accb3c7
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-00kf-9635000000-12b340bddf8bb5e19344
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-01b9-1911000000-e220e47a7de32a02498d
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	216.6330918	predicted	DarkChem Lite v0.1.0
[M-H]-	194.14165	predicted	DeepCCS 1.0 (2019)
[M+H]+	217.1474918	predicted	DarkChem Lite v0.1.0
[M+H]+	196.49965	predicted	DeepCCS 1.0 (2019)
[M+Na]+	216.6007918	predicted	DarkChem Lite v0.1.0
[M+Na]+	203.15666	predicted	DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.

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Details1. Histamine H1 receptor

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antagonist

General Function: Histamine receptor activity
Specific Function: In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name: HRH1
Uniprot ID: P35367
Uniprot Name: Histamine H1 receptor
Molecular Weight: 55783.61 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. [Article]

Details2. Voltage-dependent L-type calcium channel subunit alpha-1C

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1C
Uniprot ID: Q13936
Uniprot Name: Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight: 248974.1 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details3. Voltage-dependent L-type calcium channel subunit alpha-1D

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1D
Uniprot ID: Q01668
Uniprot Name: Voltage-dependent L-type calcium channel subunit alpha-1D
Molecular Weight: 245138.75 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details4. Voltage-dependent L-type calcium channel subunit alpha-1F

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1F
Uniprot ID: O60840
Uniprot Name: Voltage-dependent L-type calcium channel subunit alpha-1F
Molecular Weight: 220675.9 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details5. Voltage-dependent L-type calcium channel subunit alpha-1S

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1S
Uniprot ID: Q13698
Uniprot Name: Voltage-dependent L-type calcium channel subunit alpha-1S
Molecular Weight: 212348.1 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details6. Voltage-dependent T-type calcium channel subunit alpha-1G

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Scaffold protein binding
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1G
Uniprot ID: O43497
Uniprot Name: Voltage-dependent T-type calcium channel subunit alpha-1G
Molecular Weight: 262468.62 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details7. Voltage-dependent T-type calcium channel subunit alpha-1H

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Scaffold protein binding
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1H
Uniprot ID: O95180
Uniprot Name: Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight: 259160.2 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details8. Voltage-dependent T-type calcium channel subunit alpha-1I

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Voltage-gated calcium channel activity
Specific Function: Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name: CACNA1I
Uniprot ID: Q9P0X4
Uniprot Name: Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight: 245100.8 Da

References

Singh BN: The mechanism of action of calcium antagonists relative to their clinical applications. Br J Clin Pharmacol. 1986;21 Suppl 2:109S-121S. [Article]
Cohen CJ, Spires S, Van Skiver D: Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonists. J Gen Physiol. 1992 Oct;100(4):703-28. [Article]

Details9. Dopamine D2 receptor

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Other/unknown

General Function: Potassium channel regulator activity
Specific Function: Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name: DRD2
Uniprot ID: P14416
Uniprot Name: D(2) dopamine receptor
Molecular Weight: 50618.91 Da

References

Brucke T, Wober C, Podreka I, Wober-Bingol C, Asenbaum S, Aull S, Wenger S, Ilieva D, Harasko-van der Meer C, Wessely P, et al.: D2 receptor blockade by flunarizine and cinnarizine explains extrapyramidal side effects. A SPECT study. J Cereb Blood Flow Metab. 1995 May;15(3):513-8. [Article]
Kuzuhara S: [Drug-induced parkinsonism]. Nihon Rinsho. 1997 Jan;55(1):112-7. [Article]
doi:10.1007/s00415-006-3004-8 [Link]

Details10. D(1) dopamine receptor (Protein Group)

Kind: Protein group
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: G-protein coupled amine receptor activity
Specific Function: Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.

Components:

Name	UniProt ID
D(1A) dopamine receptor	P21728
D(1B) dopamine receptor	P21918

References

Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [Article]

Details11. Muscarinic acetylcholine receptor (Protein Group)

Kind: Protein group
Organism: Humans
Pharmacological action: Unknown
Actions: Binder

General Function: Phosphatidylinositol phospholipase c activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...

Components:

Name	UniProt ID
Muscarinic acetylcholine receptor M1	P11229
Muscarinic acetylcholine receptor M2	P08172
Muscarinic acetylcholine receptor M3	P20309
Muscarinic acetylcholine receptor M4	P08173
Muscarinic acetylcholine receptor M5	P08912

References

Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y: Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000 May;21(4):129-38. [Article]

Enzymes

Details1. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Narimatsu S, Kariya S, Isozaki S, Ohmori S, Kitada M, Hosokawa S, Masubuchi Y, Suzuki T: Involvement of CYP2D6 in oxidative metabolism of cinnarizine and flunarizine in human liver microsomes. Biochem Biophys Res Commun. 1993 Jun 30;193(3):1262-8. doi: 10.1006/bbrc.1993.1761. [Article]

Details2. Cytochrome P450 2C9

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2C9
Uniprot ID: P11712
Uniprot Name: Cytochrome P450 2C9
Molecular Weight: 55627.365 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [Article]

Details3. Cytochrome P450 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP1A2
Uniprot ID: P05177
Uniprot Name: Cytochrome P450 1A2
Molecular Weight: 58293.76 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [Article]
Zhou SF, Yang LP, Zhou ZW, Liu YH, Chan E: Insights into the substrate specificity, inhibitors, regulation, and polymorphisms and the clinical impact of human cytochrome P450 1A2. AAPS J. 2009 Sep;11(3):481-94. doi: 10.1208/s12248-009-9127-y. Epub 2009 Jul 10. [Article]

Details4. Cytochrome P450 2B6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2B6
Uniprot ID: P20813
Uniprot Name: Cytochrome P450 2B6
Molecular Weight: 56277.81 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [Article]

Details5. Cytochrome P450 2A6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name: CYP2A6
Uniprot ID: P11509
Uniprot Name: Cytochrome P450 2A6
Molecular Weight: 56501.005 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [Article]

Details6. Cytochrome P450 1A1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Vitamin d 24-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP1A1
Uniprot ID: P04798
Uniprot Name: Cytochrome P450 1A1
Molecular Weight: 58164.815 Da

References

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [Article]

Details7. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Uesawa Y, Takeuchi T, Mohri K: Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17. [Article]

Carriers

Details1. Serum albumin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Regulator

General Function: Toxic substance binding
Specific Function: Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name: ALB
Uniprot ID: P02768
Uniprot Name: Serum albumin
Molecular Weight: 69365.94 Da

References

Martinez-Gomez MA, Carril-Aviles MM, Sagrado S, Villanueva-Camanas RM, Medina-Hernandez MJ: Characterization of antihistamine-human serum protein interactions by capillary electrophoresis. J Chromatogr A. 2007 Apr 20;1147(2):261-9. doi: 10.1016/j.chroma.2007.02.054. Epub 2007 Feb 22. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 02, 2023 06:52

Cinnarizine

Identification

Structure for Cinnarizine (DB00568)

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Properties

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Components:

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Enzymes

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