General Information of Drug (ID: DMUJ94B)

Drug Name
A-68930 Drug Info
Synonyms
5,6-Dihydroxy-3-phenyl-1-aminomethylisochroman; A-70108; A 68930; A70360; A70108; A68930; A 70360; A-70360; A 70108; UNII-B4NI77O5D4; CHEMBL86931; B4NI77O5D4; 1-(Aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran; 130465-45-1; 1H-2-Benzopyran-5,6-diol, 1-(aminomethyl)-3,4-dihydro-3-phenyl-, (1R-cis)-; Tocris-1534; AC1L3UDV; GTPL6077; SCHEMBL10380334; CHEBI:103966; ZINC3787668; BDBM50007129; NCGC00025206-01; NCGC00025206-02; LS-172768; BRD-K33400588-003-01-2
Indication
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Terminated [1]
Cross-matching ID
PubChem CID
122324
ChEBI ID
CHEBI:103966
CAS Number
CAS 130465-45-1
TTD Drug ID
DMUJ94B

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug(s) Targeting Dopamine D1 receptor (D1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenyltoloxamine DMKAEQW Allergy 4A80-4A85 Approved [5]
Pergolide DM14MAE Parkinson disease 8A00.0 Approved [6]
Methylergonovine DMBEX4O Spontaneous abortion JA00.0 Approved [7]
Fenoldopam DMFAOKP Hypertension BA00-BA04 Approved [8]
Zicronapine DMP8ESD Schizophrenia 6A20 Phase 3 [9]
Ecopipam DMS9R43 Cocaine addiction 6C45.2 Phase 3 [10]
DAS-431 DMM3BPL Dementia 6D80-6D86 Phase 2 [11]
Dihydrexidine DMACPQO Psychotic disorder 6A20-6A25 Phase 1/2 [12]
Lu AF28996 DMY572G Parkinson disease 8A00.0 Phase 1 [13]
BAM-1110 DMPMKUF Parkinson disease 8A00.0 Discontinued in Phase 2 [14]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [15]
Haloperidol DM96SE0 Delirium Approved [16]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [17]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [18]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [19]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [20]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [21]
Pimozide DMW83TP Schizophrenia 6A20 Approved [22]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [23]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By D(1A) dopamine receptor (DRD1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [25]
Haloperidol DM96SE0 Delirium Approved [26]
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [27]
Pergolide mesylate DM5GKOV N. A. N. A. Approved [28]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [26]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [29]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [30]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [31]
Methamphetamine DMPM4SK Anxiety Approved [32]
Clozapine DMFC71L Schizophrenia 6A20 Approved [33]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine D1 receptor (D1R) TTZFYLI DRD1_HUMAN Modulator [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Inhibitor [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
D(1A) dopamine receptor (DRD1) OTLZPBT7 DRD1_HUMAN Protein Interaction/Cellular Processes [4]

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: 6077).
2 Comparison of the D1-dopamine agonists SKF-38393 and A-68930 in neonatal 6-hydroxydopamine-lesioned rats: behavioral effects and induction of c-fos-like immunoreactivity. J Pharmacol Exp Ther. 1992 Aug;262(2):855-65.
3 (1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist. J Med Chem. 1990 Nov;33(11):2948-50.
4 Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists. Mol Pharmacol. 2005 Oct;68(4):1039-48. doi: 10.1124/mol.105.012153. Epub 2005 Jun 28.
5 Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
7 Reinforcement in an in vitro analog of appetitive classical conditioning of feeding behavior in Aplysia: blockade by a dopamine antagonist. Learn Mem. 2005 May-Jun;12(3):216-20.
8 Etiology of iodinated radiocontrast nephrotoxicity and its attenuation by beraprost. Yakugaku Zasshi. 2008 Jul;128(7):1023-9.
9 Clinical pipeline report, company report or official report of Lundbeck.
10 A D1 receptor antagonist, ecopipam, for treatment of tics in Tourette syndrome.Clin Neuropharmacol.2014 Jan-Feb;37(1):26-30.
11 Adrogolide HCl (ABT-431; DAS-431), a prodrug of the dopamine D1 receptor agonist, A-86929: preclinical pharmacology and clinical data. CNS Drug Rev. 2001 Fall;7(3):305-16.
12 trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization o... J Med Chem. 2006 Nov 16;49(23):6848-57.
13 Clinical pipeline report, company report or official report of Lundbeck
14 Therapeutic effects of dopamine D1/D2 receptor agonists on detrusor hyperreflexia in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned parkinso... J Pharmacol Exp Ther. 1998 Jul;286(1):228-33.
15 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
16 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
17 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
18 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
19 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
20 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: 3639).
21 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
22 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
23 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
24 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
25 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
26 Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95.
27 Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. Relation to extrapyramidal side effects. Arch Gen Psychiatry. 1992 Jul;49(7):538-44. doi: 10.1001/archpsyc.1992.01820070032005.
28 Pergolide is an inhibitor of voltage-gated potassium channels, including Kv1.5, and causes pulmonary vasoconstriction. Circulation. 2005 Sep 6;112(10):1494-9. doi: 10.1161/CIRCULATIONAHA.105.556704. Epub 2005 Aug 29.
29 Dopamine-mediated inhibition of renal Na+/K+-ATPase in HK-2 cells is reduced by ouabain. Clin Exp Pharmacol Physiol. 2010 May;37(5-6):613-8. doi: 10.1111/j.1440-1681.2010.05364.x. Epub 2010 Feb 4.
30 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
31 Characterizing fucoxanthin as a selective dopamine D(3)/D(4) receptor agonist: Relevance to Parkinson's disease. Chem Biol Interact. 2019 Sep 1;310:108757. doi: 10.1016/j.cbi.2019.108757. Epub 2019 Jul 16.
32 Dopamine D1 receptor protein is elevated in nucleus accumbens of human, chronic methamphetamine users. Mol Psychiatry. 2000 Nov;5(6):664-72. doi: 10.1038/sj.mp.4000760.
33 Association study of four dopamine D1 receptor gene polymorphisms and clozapine treatment response. J Psychopharmacol. 2007 Sep;21(7):718-27. doi: 10.1177/0269881106072341. Epub 2006 Nov 8.