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

General Information of Drug (ID: DMMUOLJ)

Drug Name

Varenicline Drug Info

Synonyms

CP 526555; Champix (TN); Chantix (TN); Varenicline (INN); 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine; 7,8,9,10-tetrahydro-6h-6,10-methanoazepino[4,5-g]quinoxaline

Indication

Disease Entry	ICD 11	Status	REF
Drug dependence		Approved	[1]
Smoking dependence	6C4A.2	Approved	[2]

Cross-matching ID

PubChem CID: 170361
CAS Number: CAS 249296-44-4
TTD Drug ID: DMMUOLJ
VARIDT Drug ID: DR00237
ACDINA Drug ID: D00722

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2)	TTL1ATN	ACHA4_HUMAN; ACHB2_HUMAN	Modulator	[3]

------------------------------------------------------------------------------------

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Organic cation transporter 1 (SLC22A1)	DTT79CX	S22A1_HUMAN	Approved	[4]
Organic cation transporter 2 (SLC22A2)	DT9IDPW	S22A2_HUMAN	Approved	[5]

------------------------------------------------------------------------------------

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2)	DTT	CHRNA4-CHRNB2	4.409	3.585	4.385	4.591
Organic cation transporter 1 (SLC22A1)	DTP	`OCT1	10.261	4.162	4.07	3.797
Organic cation transporter 2 (SLC22A2)	DTP	`OCT2	3.766	3.548	7.303	3.548

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

Drug dependence

ICD Disease Classification

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2)	DTT	CHRNA4-CHRNB2	3.51E-10	-0.15	-0.61
Organic cation transporter 1 (SLC22A1)	DTP	SLC22A1	8.54E-01	1.24E-02	7.20E-02
Organic cation transporter 2 (SLC22A2)	DTP	SLC22A2	8.22E-01	-1.05E-02	-3.83E-02

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Varenicline FDA Label
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. (Ligand id: 5459).
3	2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
4	Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2. J Med Chem. 2013 Sep 26;56(18):7232-42.
5	Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: an in vitro-in vivo study. Clin Pharmacol Ther. 2008 Apr;83(4):567-76.