A dual histamine H1 and muscarinic acetylcholine receptor antagonist
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Mequitazine

Item No. 45325

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
10-(1-azabicyclo[2.2.2]oct-3-ylmethyl)-10H-phenothiazine
CAS Number
29216-28-2
Synonyms
  • NSC 303612
Molecular Formula
C20H22N2S
Formula Weight
322.5
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
C1(SC2=C(C=CC=C2)N3CC4CN5CCC4CC5)=C3C=CC=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $91

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    25 mg

    $146

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    50 mg

    $228

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    Product Description

    Mequitazine is a dual antagonist of histamine H1 and muscarinic acetylcholine receptors (Kis = 4.4 and 5 nM, respectively).1 In vivo, oral or subcutaneous administration of mequitazine increases survival in a rat model of mast cell degranulation induced by compound 48/80 (Item No. 22173; ED50s = 1.02 and 0.26 mg/kg, respectively).2 Formulations containing mequitazine have been used in the treatment of urticaria and allergic rhinitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kubo, N., Shirakawa, S., Kuno, T., et al. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptor-binding assay. Jpn. J. Pharmacol. 43(3), 277-282 (1987).

    2. Neimegeers, C.J.E., Awouters, F.H.L., and Janssen, P.A.J. The in vivo pharmacological profile of histamine (H1) antagonists in the rat. Drug Dev. Res. 2, 559-566 (1982).