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Description: Chlorprothixene (Paxyl; Rentovet; Truxal; Ro 4-0403; N-714; MK-184; Taractan; Tarasan), an typical antipsychotic drug of the thioxanthene class, is an antagonist of dopamine and histamine receptors with potential antipsychotic, sedative and antiemetic activity. It inhibits dopamine receptors D1, D2, D3, D5, histamin receptors H1, 5-HT2, serotonin receptors 5-HT6/7 with Ki values of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.
References: Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42; J Pharmacol Exp Ther. 1961 Jul;133:18-24.
Related CAS #: 6469-93-8 (HCl) 113-59-7 (free base)
Chemical Name: 1-Propanamine, 3-(2-chloro-9H-thioxanthen-9-ylidene)-N,N-dimethyl-, (Z)-
InChi Key: WSPOMRSOLSGNFJ-AUWJEWJLSA-N
InChi Code: InChI=1S/C18H18ClNS/c1-20(2)11-5-7-14-15-6-3-4-8-17(15)21-18-10-9-13(19)12-16(14)18/h3-4,6-10,12H,5,11H2,1-2H3/b14-7-
SMILES Code: CN(C)CC/C=C1C2=C(SC3=C\1C=CC=C3)C=CC(Cl)=C2
MK 184; N 714; N 714C; NSC 1872;0 Paxyl; Rentovet; Ro 4-0403; N-714; MK-184; Taractan; Tarasan; Chlorprothixene
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Chlorprothixene exerts strong binding affinities to the dopamine and histamine receptors, such as D1, D2, D3, D5 and H1 with Ki values of 18nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM, respectively, but has little affinity to H3 (Ki >1000 nM). Chlorprothixene also shows high affinities for both rat 5-HT6 from stably transfected HEK-293 cells, and rat 5-HT7 receptors from transiently expressed COS-7 cells, with Ki values of 3 nM and 5.6 nM, respectively. Administration of chlorprothixene results in inhibition of SARS-CoV replication in Vero 76 cells, with IC50 of 16.7 μM for Urbani strain, 13.0 μM for Frankfurt-1, 18.5 μM for CHUK-W1 and 15.8 μM for Toronto-2. There are similar to those detected with promazine.
Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42; J Pharmacol Exp Ther. 1961 Jul;133:18-24.
Purity ≥98%
COA
MSDS