A histamine H1 receptor antagonist
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Trimeprazine (tartrate)

Item No. 33891

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N,β-trimethyl-10H-phenothiazine-10-propanamine, 2R,3R-dihydroxybutanedioate
CAS Number
4330-99-8
Synonyms
  • Alimemazine
  • NSC 17475
Molecular Formula
C18H22N2S • 1/2C4H6O6
Formula Weight
373.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): insol
λmax
252 nm
SMILES
CN(C)CC(C)CN1C2=CC=CC=C2SC3=CC=CC=C31.OC([C@H](O)[C@@H](O)C(O)=O)=O
InChi Code
InChI=1S/2C18H22N2S.C4H6O6/c2*1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)21-18-11-7-5-9-16(18)20;5-1(3(7)8)2(6)4(9)10/h2*4-11,14H,12-13H2,1-3H3;1-2,5-6H,(H,7,8)(H,9,10)/t;;1-,2-/m..1/s1
InChi Key
AJZJIYUOOJLBAU-CEAXSRTFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Trimeprazine is a histamine H1 receptor antagonist (Ki = 0.72 nM in a radioligand binding assay).1 It is selective for the histamine H1 receptor over muscarinic acetylcholine receptors (mAChRs; Ki = 38 nM in a radioligand binding assay). Trimeprazine inhibits anti-IgE-induced histamine release from isolated human lung fragments (IC50 = 19 nM) but induces histamine release with a 50% release concentration (RC50) of 1.03 µM.2 It reduces severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.76 µM) with a 50% cytotoxic concentration (CC50) value of 19.73 µM.3 Formulations containing trimeprazine have been used in the treatment of allergic pruritis and motion sickness.

    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. Church, M.K., and Gradidge, C.F. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br. J. Pharmacol. 69(4), 663-667 (2019).

    3. Yang, L., Pei, R.-J., Li, H., et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol. Sin. 42(8), 1347-1353 (2020).