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

General Information of Drug (ID: DMCME17)

Drug Name

Lisuride Drug Info

Synonyms

Lisurida; Lisuridum; Lysurid; Lysuride; Lisuride [INN]; Lysuride Hydrogen Maleate; Methylergol Carbamide; Arolac (TN); Cuvalit (TN); Dipergon (TN); Dopergin (TN); Dopergine (TN); Lisurida [INN-Spanish]; Lisuride (INN); Lisuridum [INN-Latin]; Lysenyl Forte (TN); Prolacam (TN); Revanil (TN); Lisuride Maleate (1:1); N'-((8alpha)-9,10-Didehydro-6-methylergolin-8-yl)-N,N-diethylurea; 1,1-diethyl-3-[(8alpha)-6-methyl-9,10-didehydroergolin-8-yl]urea; 3-(9,10-Didehydro-6-methylergolin-8alpha-yl)-1,1-diethylurea

Indication

Disease Entry	ICD 11	Status	REF
Parkinson disease	8A00.0	Approved	[1] , [2]
Fibrosis	GA14-GC01	Phase 3	[3]

Therapeutic Class

Antiparkinson Agents

Cross-matching ID

PubChem CID: 28864
ChEBI ID: CHEBI:51164
CAS Number: CAS 18016-80-3
TTD Drug ID: DMCME17
INTEDE Drug ID: DR0965

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Dopamine D2 receptor (D2R)	TTEX248	DRD2_HUMAN	Agonist	[4] , [5] , [6]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Phase 3	[7]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Phase 3	[7]

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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
Dopamine D2 receptor (D2R)	DTT	DRD2	5.345	5.634	5.789	5.901
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

Parkinson disease

ICD Disease Classification

8A00.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Dopamine D2 receptor (D2R)	DTT	DRD2	2.50E-02	-0.08	-0.49
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	7.30E-01	-1.91E-02	-1.41E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.04E-02	6.29E-02	3.54E-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: 43).
2	Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis. Clin Neuropharmacol. 2006 Mar-Apr;29(2):80-6.
3	ClinicalTrials.gov (NCT00408915) Continuous Application of Lisuride in Parkinson's Disease by Subcutaneous Infusion. U.S. National Institutes of Health.
4	Fibrotic heart-valve reactions to dopamine-agonist treatment in Parkinson's disease. Lancet Neurol. 2007 Sep;6(9):826-9.
5	Medical management of levodopa-associated motor complications in patients with Parkinson's disease. CNS Drugs. 2007;21(8):677-92.
6	Tolerance to some behavioural effects of lisuride, a dopamine receptor agonist, and reverse tolerance to others, after repeated administration. Neuropharmacology. 1985 Mar;24(3):199-206.
7	Stable expression of human cytochrome P450 3A4 in V79 cells and its application for metabolic profiling of ergot derivatives. Eur J Pharmacol. 1995 Oct 6;293(3):183-90.