Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM51FY6)

Drug Name

Tacrine Drug Info

Synonyms

Cognex; Romotal; Tacrina; Tacrinal; Tacrinum; Tenakrin; Tetrahydroaminacrine; Tetrahydroaminoacridine; Tetrahydroaminocrin; Tetrahydroaminocrine; Tha; Tacrine hydrochloride; BBL001044; CS 12602; Cognex (TN); Tacrina [INN-Spanish]; Tacrinal (TN); Tacrine (INN); Tacrine [INN:BAN]; Tacrinum [INN-Latin]; 1,2,3,4-TETRAHYDRO-9-ACRIDINAMINE; 1,2,3,4-TETRAHYDRO-9-ACRIDINAMINE (SEE ALSO 1684-40-8); 1,2,3,4-Tetrahydro-9-acridineamine; 1,2,3,4-Tetrahydro-acridin-9-ylamine; 1,2,3,4-Tetrahydroaminoacridine; 1,2,3,4-tetrahydroacridin-9-amine; 5-Amino-6,7,8,9-tetrahydroacridine (European); 9-AMINOTETRAHYDROACRIDINE; 9-Acridinamine, 1,2,3,4-tetrahydro-(9CI); 9-Amino-1,2,3,4-Tetrahydroacridine Hydrate Hydrochloride Hydrate; 9-amino-1,2,3,4-tetrahydroacridine

Indication

Disease Entry	ICD 11	Status	REF
Alzheimer disease	8A20	Approved	[1]

Therapeutic Class

Parasympathomimetics

Cross-matching ID

PubChem CID: 1935
ChEBI ID: CHEBI:45980
CAS Number: CAS 321-64-2
TTD Drug ID: DM51FY6
VARIDT Drug ID: DR00183
INTEDE Drug ID: DR1523

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Acetylcholinesterase (AChE)	TT1RS9F	ACES_HUMAN	Inhibitor	[2]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Glutathione S-transferase alpha-1 (GSTA1)	DE4ZHS1	GSTA1_HUMAN	Approved	[4]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[5]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Acetylcholinesterase (AChE)	DTT	ACHE	1.678	1.926	1.766	5.252
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Glutathione S-transferase alpha-1 (GSTA1)	DME	GSTA1	10.53	6.221	8.589	9.978

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Alzheimer disease

ICD Disease Classification

8A20

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Acetylcholinesterase (AChE)	DTT	ACHE	6.39E-02	-1.07	-1.15
P-glycoprotein 1 (ABCB1)	DTP	P-GP	6.54E-01	1.95E-01	4.04E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	8.46E-01	-6.63E-03	-4.49E-02
Glutathione S-transferase alpha-1 (GSTA1)	DME	GSTA1	5.78E-01	3.39E-02	1.54E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6687).
2	Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19.
3	Tacrine sinusoidal uptake and biliary excretion in sandwich-cultured primary rat hepatocytes. J Pharm Pharm Sci. 2014;17(3):427-38.
4	Combined glutathione-S-transferase M1 and T1 genetic polymorphism and tacrine hepatotoxicity. Clin Pharmacol Ther. 2000 Apr;67(4):432-7.
5	Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218.