MIZOLASTINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H25FN6O
Molecular Weight	432.4933
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C1CCN(CC1)C2=NC3=C(C=CC=C3)N2CC4=CC=C(F)C=C4)C5=NC=CC(=O)N5

InChI

InChIKey=PVLJETXTTWAYEW-UHFFFAOYSA-N

InChI=1S/C24H25FN6O/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32)

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/18020585
Curator's Comment: description was created based on several sources, including http://www.medicines.org.uk/emc/medicine/19970/SPC/Mizollen+10+mg+modified-release+tablets

Mizolastine (Mizollen) is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. It blocks H1 receptors and is commonly fast-acting. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 315 Target ID: CHEMBL231 Sources: http://www.ncbi.nlm.nih.gov/pubmed/7612054	Antagonist 2778		47.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Seasonal allergic rhinoconjunctivitis 1 Sources: http://www.medicines.org.uk/emc/medicine/19970/SPC/Mizollen+10+mg+modified-release+tablets	Primary		Approved 8429	Mizollen Approved Use Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. Launch Date 2003
Chronic idiopathic urticaria 11 Sources: http://www.ncbi.nlm.nih.gov/pubmed/16278258	Primary		Approved 8429	Mizollen Approved Use Mizolastine is a long-acting H1 -antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria. Launch Date 2003

PubMed

Title	Date	PubMed
In vivo and in vitro interaction of the novel selective histamine H1 receptor antagonist mizolastine with H1 receptors in the rodent.	1995 May	7612054
Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria.	1998 Jul	18020585
Efficacy and safety of mizolastine 10 mg in a placebo-controlled comparison with loratadine in chronic idiopathic urticaria: results of the MILOR Study.	1999 Jan	10188144
Antiallergic effects of H1-receptor antagonists.	2000	11291777
Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine.	2000 Nov	11082114
Cetirizine and loratadine: minimal risk of QT prolongation.	2010 Feb	20455340

Patents

Sample Use Guides

In Vivo Use Guide

10 mg daily was administered for 14 days during the pollen season

Route of Administration: Oral

In Vitro Use Guide

The highest dose of mizolastine (6 x 10(-6) M), corresponding to 10-fold the peak plasma level after a single oral administration of 10 mg, was able to act on fibroblasts, significantly downregulating the expression of CD54 (p<0.05). Regarding T lymphocyte proliferation, the addition of mizolastine did not induce any significant change; furthermore, mizolastine was ineffective at all of the tested concentrations on both HLA-DR expression and CD4+/CD8+ ratio.

Name

Type

Language

MIZOLASTINE

Official Name

English

MIZOLLEN

Brand Name

English

mizolastine [INN]

Common Name

English

MIZOLASTINE [MI]

Common Name

English

MIZOLASTINE [MART.]

Common Name

English

2-((1-(1-(P-FLUOROBENZYL)-2-BENZIMIDAZOLYL)-4-PIPERIDYL)METHYLAMINO)-4(3H)-PYRIMIDINONE

Common Name

English

Mizolastine [WHO-DD]

Common Name

English

MIZOLASTINE [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29578