P-10358

Smith et al. IC50 0.10 microM for AChE 0.08 microM for BChE selectivity 1.25 11 time less potent than heptastigmine and 2.5 more potent than Tacrine

General

Type : Carbamate,Indole,Pyridine

Chemical_Nomenclature : [1-[(3-fluoropyridin-4-yl)amino]-3-methylindol-5-yl] N-methylcarbamate

Canonical SMILES : CC1=CN(C2=C1C=C(C=C2)OC(=O)NC)NC3=C(C=NC=C3)F

InChI : InChI=1S\/C16H15FN4O2\/c1-10-9-21(20-14-5-6-19-8-13(14)17)15-4-3-11(7-12(10)15)23-16(22)18-2\/h3-9H,1-2H3,(H,18,22)(H,19,20)

InChIKey : GUHMRCCRDRBMHO-UHFFFAOYSA-N

Other name(s) : 1-((3-Fluoro-4-pyridinyl)amino)-3-methyl-1H-indol-5-ol methylcarbamate (ester),1H-Indol-5-ol, 1-((3-fluoro-4-pyridinyl)amino)-3-methyl-, methylcarbamate (ester)


MW : 314.314

Formula : C16H15FN4O2

CAS_number : 188240-59-7

PubChem : 3075612

UniChem : GUHMRCCRDRBMHO-UHFFFAOYSA-N

IUPHAR :

Wikipedia :

Target

Families : P-10358 ligand of proteins in family: ACHE || BCHE

Stucture :

Protein :

References (2)

Title : Central and peripheral activity of cholinesterase inhibitors as revealed by yawning and fasciculation in rats - Ogura_2001_Eur.J.Pharmacol_415_157
Author(s) : Ogura H , Kosasa T , Kuriya Y , Yamanishi Y
Ref : European Journal of Pharmacology , 415 :157 , 2001
Abstract : Ogura_2001_Eur.J.Pharmacol_415_157
ESTHER : Ogura_2001_Eur.J.Pharmacol_415_157
PubMedSearch : Ogura_2001_Eur.J.Pharmacol_415_157
PubMedID: 11274994

Title : Pharmacological activity and safety profile of P10358, a novel, orally active acetylcholinesterase inhibitor for Alzheimer's disease - Smith_1997_J.Pharmacol.Exp.Ther_280_710
Author(s) : Smith CP , Bores GM , Petko W , Li M , Selk DE , Rush DK , Camacho F , Winslow JT , Fishkin R , Cunningham DM , Brooks KM , Roehr J , Hartman HB , Davis L , Vargas HM
Ref : Journal of Pharmacology & Experimental Therapeutics , 280 :710 , 1997
Abstract : Smith_1997_J.Pharmacol.Exp.Ther_280_710
ESTHER : Smith_1997_J.Pharmacol.Exp.Ther_280_710
PubMedSearch : Smith_1997_J.Pharmacol.Exp.Ther_280_710
PubMedID: 9023283