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

General Information of Drug (ID: DM4BP7S)

Drug Name

R-226161 Drug Info

Synonyms

R-226161; UNII-0878P6YAG6; CHEMBL318235; 0878P6YAG6; SCHEMBL16583684; BDBM50146518; cis-(+)-7,8-dimethoxy-3-[4-(2-methyl-3-(4-fluoro)phenyl-2(E)-propen-1-yl)piperazin-1-ylmethyl]-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole; 3H-(1)Benzopyrano(4,3-C)isoxazole, 3-((4-((2E)-3-(4-fluorophenyl)-2-methyl-2-propen-1-yl)-1-piperazinyl)methyl)-3a,4-dihydro-7,8-dimethoxy-, (cis)-(+)-; (3R,3aS)-3-{4-[3-(4-Fluoro-phenyl)-2-methyl-allyl]-piperazin-1-ylmethyl}-7,8-dimethoxy-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

PubChem CID: 16655023
CAS Number: CAS 452314-01-1
TTD Drug ID: DM4BP7S

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor alpha-1A (ADRA1A)	TTNGILX	ADA1A_HUMAN	Inhibitor	[1]
Adrenergic receptor alpha-2A (ADRA2A)	TTWG9A4	ADA2A_HUMAN	Inhibitor	[1]
Adrenergic receptor alpha-2B (ADRA2B)	TTWM4TY	ADA2B_HUMAN	Inhibitor	[1]
Adrenergic receptor alpha-2C (ADRA2C)	TT2NUT5	ADA2C_HUMAN	Inhibitor	[1]
Dopamine D3 receptor (D3R)	TT4C8EA	DRD3_HUMAN	Inhibitor	[1]
Dopamine transporter (DAT)	TTVBI8W	SC6A3_HUMAN	Inhibitor	[1]
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Inhibitor	[1]
Serotonin transporter (SERT)	TT3ROYC	SC6A4_HUMAN	Inhibitor	[1]
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Inhibitor	[1]

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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
Substance-P receptor (TACR1)	DTT	TACR1	3.597	4.186	4.271	5.113
Dopamine transporter (DAT)	DTT	SLC6A3	4	2.609	5.233	3.7
Histamine H1 receptor (H1R)	DTT	HRH1	5.972	5.7	5.816	6.002
Adrenergic receptor alpha-1A (ADRA1A)	DTT	ADRA1A	3.154	3.853	4.129	2.963
Dopamine D3 receptor (D3R)	DTT	DRD3	1.379	2.446	1.233	1.07
Serotonin transporter (SERT)	DTT	SLC6A4	6.278	5.469	6.075	6.966
Adrenergic receptor alpha-2C (ADRA2C)	DTT	ADRA2C	5.013	2.379	5.594	2.07

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

Discovery agent

ICD Disease Classification

N.A.

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Adrenergic receptor alpha-2C (ADRA2C)	DTT	ADRA2C	1.76E-01	-0.06	-0.28

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.