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

General Information of Drug (ID: DMKSQG0)

Drug Name

Tiagabine Drug Info

Synonyms

tiagabine; 115103-54-3; Gabitril; Tiagabinum; Tiagabina; (R)-Tiagabine; Tiagabinum [INN-Latin]; Tiagabina [INN-Spanish]; Tiagabine [INN:BAN]; Tiagabine [INN]; Abbott-70569; UNII-Z80I64HMNP; Tiagabine (INN); ABBOTT-70569-1; Gabitril (TN); CHEMBL1027; Z80I64HMNP; ABT-569; CHEBI:9586; NO-328; (-)-(R)-1-(4,4-Bis(3-methyl-2-thienyl)-3-butenyl)nipecotic acid; A-70569-1; (R)-1-(4,4-Bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid; Gabatril; NO 329; Gabitril; NO-329; Tiagabina [INN-Spanish];Tiagabine (INN); N-(4,4-di(3-methylthien-2-yl)but-3-enyl)nipecotic acid; (3R)-1-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]piperidine-3-carboxylic acid; (3R)-1-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid; [3H]tiagabine

Indication

Disease Entry	ICD 11	Status	REF
Epilepsy	8A60-8A68	Approved	[1]
Anxiety disorder	6B00-6B0Z	Phase 2	[1]

Therapeutic Class

Anticonvulsants

Cross-matching ID

PubChem CID: 60648
ChEBI ID: CHEBI:9586
CAS Number: CAS 115103-54-3
TTD Drug ID: DMKSQG0
VARIDT Drug ID: DR01016
INTEDE Drug ID: DR1588
ACDINA Drug ID: D00673

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
GABA transporter GAT-1 (SLC6A1)	TTPRKM0	SC6A1_HUMAN	Inhibitor	[2]
Gamma-aminobutyric acid uptake (GABAU)	TTV9MQG	NOUNIPROTAC	Inhibitor	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[4]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_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
GABA transporter GAT-1 (SLC6A1)	DTT	SLC6A1	8.477	4.548	4.194	5.53
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

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

Epilepsy

ICD Disease Classification

8A60-8A68

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
GABA transporter GAT-1 (SLC6A1)	DTT	SLC6A1	4.99E-02	-0.24	-0.62
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	6.60E-01	2.51E-02	8.26E-02
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	8.62E-03	1.37E-01	8.67E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.51E-01	8.39E-02	5.00E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.93E-04	-6.16E-01	-2.64E+00

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: 4818).
2	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. (Target id: 929).
3	Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
4	Enzyme induction and inhibition by new antiepileptic drugs: a review of human studies. Fundam Clin Pharmacol. 2000 Jul-Aug;14(4):301-19.
5	Actual and Predicted Pharmacokinetic Interactions Between Anticonvulsants and Antiretrovirals.