General Information of Drug (ID: DM6RZ9Q)

Drug Name
Clonidine Drug Info
Synonyms
clonidine; Clonidin; Duraclon; Chlornidinum; 4205-90-7; Catapres-TTS; Catarpresan; Catarpres; Adesipress; Catapres; Catapressan; Catapresan; ST 155BS; ST-155-BS; Clonidinum; Clonidina; Clonidinum [INN-Latin]; Clonidinhydrochlorid; CATAPRES-TTS-3; CATAPRES-TTS-1; CATAPRES-TTS-2; N-(2,6-Dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine; Isoglaucon; 2-(2,6-Dichloroanilino)-2-imidazoline; Dixarit; SKF 34427; Catapres- TTS; Clonidina [INN-Spanish]; M-5041T; Hemiton; CLORPRES; clonidine (amino form); Adesipress; Clofenil; Clopheline; Duraclont; Gemiton; Klofelin; Klofenil; M 5041T; Catapres (TN); Catarpres-TTS; ST-155BS; Tenso-Timelets; Catarpres-TTS (TN); Clonidine [USAN:BAN:INN]; Clonidine (JAN/USAN/INN); 1H-Imidazol-2-amine, N-(2,6-dichlorophenyl)-4,5-dihydro-(9CI); 2,6-Dichloro-N-2-imidazolidinylidenebenzenamine; 2,6-dichloro-N-(2-imidazolidinylidene)aniline; 2,6-dichloro-N-2-imidazolidinylidenebenzenamide; 2,6-dichloro-N-imidazolidin-2-ylideneaniline; 2-((2,6-Dichlorophenyl)imino)imidazolidine; 2-(2,6-Dichloroanilino)-1,3-diazacyclopentene-(2);2-(2,6-Dichloroanilino)-2-imidazoline; 2-(2,6-Dichlorophenylamino)-2-imidazoline; 2-(2,6-Dichlorophenylimino)imidazolidine; 2-Imidazoline, 2-(2,6-dichloroanilino)-(7CI,8CI); 2-[(2,6-Dichlorophenyl)imino]imidazoline; 2-[(2,6-dichlorophenyl)imino]-2-imidazoline; 734571A; 2,6-DICHLORO-N-IMIDAZOLIDIN-2-YLIDENEANILINE
Indication
Disease Entry ICD 11 Status REF
Attention deficit hyperactivity disorder 6A05.Z Approved [1]
Hypertension BA00-BA04 Approved [2]
Neonatal abstinence syndrome Approved [1]
Diabetic neuropathy 8C0Z Phase 3 [3]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
2803
ChEBI ID
CHEBI:3757
CAS Number
CAS 4205-90-7
TTD Drug ID
DM6RZ9Q
VARIDT Drug ID
DR00521
INTEDE Drug ID
DR0352
ACDINA Drug ID
D00141

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Adrenergic receptor Alpha-2 (ADRA2) TTQ8AFT NOUNIPROTAC Agonist [4]
Membrane copper amine oxidase (AOC3) TT7HC21 AOC3_HUMAN Inhibitor [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic cation transporter 3 (SLC22A3) DT6201N S22A3_HUMAN Approved [6]
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Approved [6]
Organic cation transporter 2 (SLC22A2) DT9IDPW S22A2_HUMAN Approved [6]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [8]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Approved [8]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [8]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [8]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Membrane copper amine oxidase (AOC3) DTT AOC3 7.055 8.263 6.709 7.374
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
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
Organic cation transporter 3 (SLC22A3) DTP `OCT3 5.289 1.963 3.472 3.621
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 3.307 5.005 3.921 5.327
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 Attention deficit hyperactivity disorder
ICD Disease Classification 6A05.Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Membrane copper amine oxidase (AOC3) DTT AOC3 8.36E-22 -1.03 -1.54
P-glycoprotein 1 (ABCB1) DTP P-GP 2.00E-01 2.57E-02 6.18E-02
Organic cation transporter 1 (SLC22A1) DTP SLC22A1 2.90E-01 -1.11E-01 -2.75E-01
Organic cation transporter 2 (SLC22A2) DTP SLC22A2 5.61E-04 -1.80E-01 -4.16E-01
Organic cation transporter 3 (SLC22A3) DTP SLC22A3 1.68E-07 4.84E-01 1.17E+00
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 4.87E-15 -3.01E-01 -6.41E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 5.05E-02 4.52E-01 5.39E-01
Cytochrome P450 2D6 (CYP2D6) DME CYP2D6 7.74E-01 -3.86E-02 -1.04E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.67E-01 -3.83E-03 -1.24E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Clonidine 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: 516).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Noradrenergic alpha-2 receptor agonists reverse working memory deficits induced by the anxiogenic drug, FG7142, in rats. Pharmacol Biochem Behav. 2000 Nov;67(3):397-403.
5 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
6 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
7 Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22.
8 CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6.