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Inhibitor Report for: Ethopropazine

Antiparkinsonian, anticholinergic. Inhibitor specific of BChE and used to differentiate BChE activity from AChE activity. Ethopropazine (also known as profenamine hydrochloride) is a medication derived from phenothiazine. It is primarily used as an antidyskinetic to treat parkinsonism. It is sold under the trade names Parsidol in the United States and Parsidan in Canada.


General
Type Phenothiazine, Drug, Sulfur compound
Chemical_Nomenclature 10-(2-diethylaminopropyl)phenothiazine hydrochloride
Canonical SMILES CCN(CC)C(C)CN1C2=CC=CC=C2SC3=CC=CC=C31
InChI InChI=1S/C19H24N2S/c1-4-20(5-2)15(3)14-21-16-10-6-8-12-18(16)22-19-13-9-7-11-17(19)21/h6-13,15H,4-5,14H2,1-3H3
InChIKey CDOZDBSBBXSXLB-UHFFFAOYSA-N
Other name(s) Lysivane ; Dibutil ; Parsidol ; Rodipal ; Parsitan ; Parphezin ; Phenoprpazine ; Profenamine ; RP3356 ; W-483 ; Isothazine ; Isothiazine ; Parkin ; BUW
________________________________________________________________________________________________
MW|312.5
Formula|C19H24N2S
CAS_number|522-00-9
PubChem|3290
UniChem|CDOZDBSBBXSXLB-UHFFFAOYSA-N
IUPHAR|7181
Wikipedia|Profenamine

Target
Families | Ethopropazine ligand of proteins in family: BCHE, ACHE
Stucture | 1 structure: 6EQP: Human butyrylcholinesterase in complex with ethopropazine
Protein | human-BCHE

References:
Search PubMed for references concerning: Ethopropazine

3 more
    Title: The effect of pesticides on carp (Cyprinus carpio L). Acetylcholinesterase and its biochemical characterization
    Szabo A, Nemcsok J, Asztalos B, Rakonczay Z, Kasa P, Hieu LH
    Ref: Ecotoxicology & Environmental Safety, 23:39, 1992 : PubMed

            

    Title: Polymorphism of pseudocholinesterase in Torpedo marmorata tissues: comparative study of the catalytic and molecular properties of this enzyme with acetylcholinesterase
    Toutant JP, Massoulie J, Bon S
    Ref: Journal of Neurochemistry, 44:580, 1985 : PubMed

            

    Title: Acetylcholinesterase and butyrylcholinesterase activity in the atria of the heart of adult albino rats
    Slavikova J, Vlk J, Hlavickova V
    Ref: Physiol Bohemoslov, 31:407, 1982 : PubMed

            


mouse-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 110 & 51 uM 1100 & 160 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337A 0.041 & 0.003 uM 0.13 & 0.002 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
Y337F 34 & 6 uM 330 & 86 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

mouse-BCHE
MutationKiKsiIc50SubstrateConditionPaper
WT 0.061 & 0.027 uM 0.130 & 0.076 uM - Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
mouse-ACHE110 & 51 uM1100 & 160 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074
mouse-BCHE0.061 & 0.027 uM0.130 & 0.076 uM- Acetylthiocholine 100mM NaP pH7.0 T22C Radic_1993_Biochemistry_32_12074