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Merck
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Key Documents

SML2065

Sigma-Aldrich

Mequitazine

≥98% (HPLC)

Synonyme(s) :

10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine, 10-(3-quinuclidinylmethyl) phenothiazine, LM 209, NSC 303612

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About This Item

Formule empirique (notation de Hill):
C20H22N2S
Numéro CAS:
29216-28-2
Poids moléculaire :
322.47
Code UNSPSC :
12352200

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

−20°C

InChI

1S/C20H22N2S/c1-3-7-19-17(5-1)22(18-6-2-4-8-20(18)23-19)14-16-13-21-11-9-15(16)10-12-21/h1-8,15-16H,9-14H2

Clé InChI

HOKDBMAJZXIPGC-UHFFFAOYSA-N

Actions biochimiques/physiologiques

Mequitazine is a potent, nonsedative, long-acting and selective H1 histamine receptor antagonist. Mequitazine exhibits weak anticholinergic activity.

Pictogrammes

Skull and crossbones
GHS06

Mention d'avertissement

Danger

Mentions de danger

H301

Classification des risques

Acute Tox. 3 Oral

Code de la classe de stockage

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

I Martinez-Mir et al.
The Journal of pharmacy and pharmacology, 40(9), 655-656 (1988-09-01)
The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plot were 9.95 +/- 0.44
K Nakamura et al.
The Journal of pharmacology and experimental therapeutics, 284(2), 437-442 (1998-03-07)
Mequitazine [10-(3-quinuclidinylmethyl) phenothiazine] is a long-acting and selective histamine H1-receptor antagonist that is mainly biotransformed by human liver microsomes to yield hydroxylated and S-oxidized metabolites. Mequitazine hydroxylase was inhibited by propranolol and quinidine. Lineweaver-Burk plots for the hydroxylation and the
Tatsuya Isomura et al.
PloS one, 9(12), e114336-e114336 (2014-12-17)
Second-generation antihistamines (AHs) have, in general, fewer sedative effects than the first-generation. However, important inter-drug differences remain in the degree of cognitive and/or psychomotor impairment. The extent to which a particular compound causes disruption can be conveniently compared, to all
Shigeru Hishinuma et al.
Journal of pharmacological sciences, 107(1), 66-79 (2008-05-01)
We evaluated changes in the binding properties of sedative and non-sedative histamine H1-receptor antagonists induced by internalization of H1 receptors in intact human U373 MG astrocytoma cells. Internalization of H1 receptors was induced without their degradation by treatment with 0.1

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