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Inhibitor Report for: Promethazine

Tricyclic amine-containing compound Promethazine is a phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.Promethazine is a phenothiazine derivative with antiemetic and antihistaminic properties. Promethazine antagonizes the central and peripheral effects of histamine mediated by histamine H1 receptors. The effects include bronchoconstriction, vasodilation and spasmodic contractions of gastrointestinal smooth muscle. In addition, this agent binds to muscarinic receptors, resulting in anticholinergic and antiemetic activities.


General
Type Phenothiazine, Drug, Not A/B H target, Sulfur Compound
Chemical_Nomenclature 10-[2-(dimethylamino)propyl]phenothiazine
Canonical SMILES CC(CN1C2=CC=CC=C2SC3=CC=CC=C31)N(C)C
InChI InChI=1S/C17H20N2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
InChIKey PWWVAXIEGOYWEE-UHFFFAOYSA-N
Other name(s) promethazine ; Proazamine ; Diphergan ; Promethazin ; Isophenergan ; Phenargan ; CHEMBL643 ; CHEBI:8461 ; SCHEMBL4700 ; RP-3277
________________________________________________________________________________________________
MW|320.90
Formula|C17H20N2S
CAS_number|58-33-3, 60-87-7
PubChem|4927
UniChem|PWWVAXIEGOYWEE-UHFFFAOYSA-N
IUPHAR|7282
Wikipedia|Promethazine

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

References:
Search PubMed for references concerning: Promethazine
    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 230 & 64 uM 4100 & 4100 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337A 29 & 11 uM 130 & 29 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337F 110 & 20 uM 1700 & 440 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

mouse-BCHE
MutationKiKsiIc50SubstrateConditionPaper
WT 1.4 & 0.7 uM 3.3 & 0.2 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
mouse-ACHE230 & 64 uM4100 & 4100 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHE1.4 & 0.7 uM3.3 & 0.2 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074