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

General Information of Drug (ID: DMWHEV8)

Drug Name
[3H]spiperone Drug Info
Synonyms
Spiperone; spiperone; Spiroperidol; Spiropitan; 749-02-0; Espiperona; Spiperonum; [3H]-spiperone; R 5147; Spiperonum [INN-Latin]; Espiperona [INN-Spanish]; E 525; UNII-4X6E73CJ0Q; NSC 170983; MLS000028615; Spiperone [USAN:INN:BAN:JAN]; 8-(3-(p-Fluorobenzoyl)propyl)-1-phenyl-1,3,8-triazaspiro(45)decan-4-one; 8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[45]decan-4-one; 8-(3-p-Fluorobenzoyl-1-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro(4,5)decane; EINECS 212-024-0; BRN 0632204; SMR000058674; [3H]-spiperone; SPIPERONE
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5265
ChEBI ID
CHEBI:9233
CAS Number
CAS 749-02-0
TTD Drug ID
DMWHEV8
VARIDT Drug ID
DR01493

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Inhibitor [2]
5-HT 2A receptor (HTR2A) TTJQOD7 5HT2A_HUMAN Inhibitor [3]
5-HT 6 receptor (HTR6) TTJS8PY 5HT6R_HUMAN Inhibitor [4]
5-HT 7 receptor (HTR7) TTO9X1H 5HT7R_HUMAN Inhibitor [4]
Adrenergic receptor alpha-1A (ADRA1A) TTNGILX ADA1A_HUMAN Inhibitor [5]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Antagonist [6]
Dopamine D3 receptor (D3R) TT4C8EA DRD3_HUMAN Antagonist [6]
Dopamine D4 receptor (D4R) TTE0A2F DRD4_HUMAN Antagonist [7]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_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
5-HT 1A receptor (HTR1A) DTT HTR1A 4.661 5.289 3.053 3.472
5-HT 7 receptor (HTR7) DTT HTR7 1.561 1.233 0.848 1.485
Adrenergic receptor alpha-1A (ADRA1A) DTT ADRA1A 3.154 3.853 4.129 2.963
5-HT 6 receptor (HTR6) DTT HTR6 5.594 5.781 5.271 3.963
5-HT 2A receptor (HTR2A) DTT HTR2A 4.84 4.904 4.652 4.129
Dopamine D2 receptor (D2R) DTT DRD2 5.345 5.634 5.789 5.901
Dopamine D4 receptor (D4R) DTT DRD4 2.138 1.766 1.322 1
Dopamine D3 receptor (D3R) DTT DRD3 1.379 2.446 1.233 1.07
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
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
5-HT 1A receptor (HTR1A) DTT HTR1A 1.49E-05 -0.22 -0.58
5-HT 6 receptor (HTR6) DTT HTR6 1.23E-05 -0.12 -0.71
Dopamine D2 receptor (D2R) DTT DRD2 2.50E-02 -0.08 -0.49
P-glycoprotein 1 (ABCB1) DTP P-GP 9.39E-02 1.07E-01 2.80E-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: 3300).
2 Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. J Med Chem. 1993 Oct 15;36(21):3161-5.
3 Activity of Parthenolide at 5HT2A receptors. J Nat Prod. 1997 Jun;60(6):651-3.
4 Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812.
5 Pharmacophore identification of alpha(1A)-adrenoceptor antagonists. Bioorg Med Chem Lett. 2005 Feb 1;15(3):657-64.
6 Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol. 2000 Jul;130(5):1045-59.
7 Differential effects of [3H]nemonapride and [3H]spiperone binding on human dopamine D4 receptors. Neurosci Lett. 1995 Feb 17;186(2-3):145-8.
8 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.