SML2065

Sigma-Aldrich

Mequitazine

≥98% (HPLC)

Synonyme(s):
10-(3-quinuclidinylmethyl) phenothiazine, LM 209, 10-(1-Azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine, NSC 303612
Empirical Formula (Hill Notation):
C20H22N2S
Numéro CAS:
Poids moléculaire:
322.47

Essai/Dosage

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Temp. 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

InChI key

HOKDBMAJZXIPGC-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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

Pictograms

Skull and crossbones

Mention d'avertissement

Danger

Mentions de danger

Conseils de prudence

RID ADR

UN 2811 6.1 / PGIII

WGK Allemagne

WGK 3

Flash Point(F)

Not applicable

Point d'éclair C

Not applicable

Certificat d'analyse
Certificat d'origine
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...
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...
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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