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Inhibitor Report for: Chlorpromazine

The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking dopamine receptors. It is one of the most sedating of the typical antipsychotics and also causes antimuscarinic effects. Tricyclic amine-containing compound


General
Type Not A/B H target, Phenothiazine, Multitarget, Drug, Sulfur Compound
Chemical_Nomenclature 8-chlorpromazine, 2-chloro-N,N-dimethyl-10H-Phenothiazine-10-propanamine
Canonical SMILES CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
InChI InChI=1S/C17H19ClN2S/c1-19(2)10-5-11-20-14-6-3-4-7-16(14)21-17-9-8-13(18)12-15(17)20/h3-4,6-9,12H,5,10-11H2,1-2H3
InChIKey ZPEIMTDSQAKGNT-UHFFFAOYSA-N
Other name(s) Propaphenin ; Largactil ; Thorazin ; Contomin ; Megaphen ; Cromedazine ; Plegomazin ; Chloropromazine ; Chlorderazin ; Thorazine ; Ormazine ; Thor-prom
________________________________________________________________________________________________
MW|355.3-318.86
Formula|C17H19ClN2S
CAS_number|69-09-0, 50-53-3
PubChem|2726
UniChem|ZPEIMTDSQAKGNT-UHFFFAOYSA-N
IUPHAR|83
Wikipedia|Chlorpromazine

Target
Families | Chlorpromazine ligand of proteins in family: ACHE, BCHE

References:
Search PubMed for references concerning: Chlorpromazine

3 more
    Title: Three distinct domains in the cholinesterase molecule confer selectivity for acetyl- and butyrylcholinesterase inhibitors
    Radic Z, Pickering NA, Vellom DC, Camp S, Taylor P
    Ref: Biochemistry, 32:12074, 1993 : PubMed

            

    Title: Differential inhibition of plasma cholinesterase variants using the dibutyrate analogue of pancuronium bromide
    Whittaker M, Britten JJ
    Ref: Hum Hered, 31:242, 1981 : PubMed

            

    Title: The activity of various esterase inhibitors towards atypical human serum cholinesterase
    Kalow W, Davies R0
    Ref: Biochemical Pharmacology, 1:183, 1958 : PubMed

            


human-BCHE
MutationKiKsiIc50SubstrateConditionPaper
D70G - - 74 uM   Lockridge_1990_Pharmacol.Ther_47_35
WT - - 4.4 uM   Lockridge_1990_Pharmacol.Ther_47_35

mouse-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 26 & 8 uM 410 & 290 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337A 17 & 7 uM 91 & 38 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337F 22 & 11 uM 540 & 191 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

mouse-BCHE
MutationKiKsiIc50SubstrateConditionPaper
WT 2.1 & 0.9 uM 8.5 & 4.0 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
human-BCHE--4.4 uM  Lockridge_1990_Pharmacol.Ther_47_35
mouse-ACHE26 & 8 uM410 & 290 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHE2.1 & 0.9 uM8.5 & 4.0 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074