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Inhibitor Report for: Promazine

Chlorpromazine was the first antipsychotic drug to be discovered. It is one of the most sedating of the typical antipsychotics and also causes antimuscarinic effects.Tricyclic amine-containing compound. Promazine is a phenothiazine with actions similar to Chlorpromazine but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.


General
Type Phenothiazine, Drug, Sulfur Compound, Not A/B H target
Chemical_Nomenclature 10-[3-(dimethylamino)propyl]phenothiazine
Canonical SMILES CN(C)CCCN1C2=CC=CC=C2SC3=CC=CC=C31
InChI InChI=1S/C17H20N2S/c1-18(2)12-7-13-19-14-8-3-5-10-16(14)20-17-11-6-4-9-15(17)19/h3-6,8-11H,7,12-13H2,1-2H3
InChIKey ZGUGWUXLJSTTMA-UHFFFAOYSA-N
Other name(s)
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MW|320.9
Formula|C17H20N2S
CAS_number|53-60-1
PubChem|4926
UniChem|ZGUGWUXLJSTTMA-UHFFFAOYSA-N
IUPHAR|7281
Wikipedia|Promazine

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

References:
Search PubMed for references concerning: Promazine
    Title: Inhibition of butyrylcholinesterase by phenothiazine derivatives
    Debord J, Merle L, Bollinger JC, Dantoine T
    Ref: J Enzyme Inhib Med Chem, 17:197, 2002 : PubMed

            

    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

            


mouse-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 50 & 10 uM 790 & 230 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337A 37 & 11 uM 150 & 27 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337F 51 & 12 uM 850 & 21 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

mouse-BCHE
MutationKiKsiIc50SubstrateConditionPaper
WT 1.8 & 0.7 uM 7.1 & 3.9 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
mouse-ACHE50 & 10 uM790 & 230 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHE1.8 & 0.7 uM7.1 & 3.9 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074