DT-Web

DB04842 - Fluspirilene


Identification
Name Fluspirilene
Accession Number DB04842
Type small molecule
Description A long-acting injectable antipsychotic agent used for chronic schizophrenia.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 475.5727
Groups approved
Monoisotopic Weight 475.243519039
Pharmacology
Indication Used for the treatment of schizophrenia.
Mechanism of action Not Available
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions
  • Avoid alcohol.

Targets


D(2) dopamine receptor
Name D(2) dopamine receptor
Gene Name DRD2
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
  • Wang SJ: Inhibition of glutamate release by fluspirilene in cerebrocortical nerve terminals (synaptosomes). Synapse. 2002 Apr;44(1):36-41. - Pubmed
  • Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE: Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73. - Pubmed
DTHybrid score 0.3321
5-hydroxytryptamine 2A receptor
Name 5-hydroxytryptamine 2A receptor
Gene Name HTR2A
Pharmacological action unknown
Actions antagonist
References
  • Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE: Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73. - Pubmed
DTHybrid score 0.274
Voltage-dependent calcium channel gamma-1 subunit
Name Voltage-dependent calcium channel gamma-1 subunit
Gene Name CACNG1
Pharmacological action unknown
Actions inhibitor
References
  • Kenny BA, Fraser S, Kilpatrick AT, Spedding M: Selective antagonism of calcium channel activators by fluspirilene. Br J Pharmacol. 1990 Jun;100(2):211-6. - Pubmed
  • Wang SJ: Inhibition of glutamate release by fluspirilene in cerebrocortical nerve terminals (synaptosomes). Synapse. 2002 Apr;44(1):36-41. - Pubmed
DTHybrid score 0.2652

Predictions


Id Partner name Gene Name Score
23 D(1A) dopamine receptor DRD1 0.1272
4119 Cytochrome P450 2D6 CYP2D6 0.1158
4512 Cytochrome P450 3A4 CYP3A4 0.0842
320 5-hydroxytryptamine 1A receptor HTR1A 0.0831
590 5-hydroxytryptamine 2C receptor HTR2C 0.0809
638 D(3) dopamine receptor DRD3 0.076
556 Alpha-1A adrenergic receptor ADRA1A 0.0755
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.06
432 D(4) dopamine receptor DRD4 0.0591
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0581
318 Alpha-2A adrenergic receptor ADRA2A 0.0567
6107 Cytochrome P450 3A7 CYP3A7 0.0554
4118 Cytochrome P450 3A5 CYP3A5 0.0546
1588 Multidrug resistance protein 1 ABCB1 0.0533
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.051
632 Alpha-1B adrenergic receptor ADRA1B 0.0463
4200 Cytochrome P450 1A2 CYP1A2 0.0454
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0451
163 D(1B) dopamine receptor DRD5 0.0448
436 5-hydroxytryptamine 2B receptor HTR2B 0.044
378 Alpha-2C adrenergic receptor ADRA2C 0.0434
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0429
716 5-hydroxytryptamine 7 receptor HTR7 0.0425
629 Alpha-2B adrenergic receptor ADRA2B 0.0422
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0421
492 Histamine H1 receptor HRH1 0.0398
725 5-hydroxytryptamine 1D receptor HTR1D 0.0346
4757 Cytochrome P450 2C9 CYP2C9 0.0319
885 5-hydroxytryptamine 1B receptor HTR1B 0.0311
6016 Cytochrome P450 2C19 CYP2C19 0.0297
1256 5-hydroxytryptamine 6 receptor HTR6 0.027
824 Sodium-dependent serotonin transporter SLC6A4 0.0264
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0261
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0251
274 Muscarinic acetylcholine receptor M5 CHRM5 0.025
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0243
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0242
6145 Solute carrier family 22 member 1 SLC22A1 0.0241
751 Potassium channel subfamily K member 6 KCNK6 0.0238
789 Alpha-1D adrenergic receptor ADRA1D 0.0236
4924 Cytochrome P450 2C8 CYP2C8 0.0223
540 Sodium-dependent noradrenaline transporter SLC6A2 0.022
172 Potassium channel subfamily K member 1 KCNK1 0.0214
174 Sigma 1-type opioid receptor SIGMAR1 0.0194
587 Serum albumin ALB 0.0193
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0188
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0188
94 5-hydroxytryptamine 4 receptor HTR4 0.0185
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0177
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0159
4160 Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2 0.0157
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0155
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0154
6013 Cytochrome P450 2E1 CYP2E1 0.015
923 Glutamate receptor 3 GRIA3 0.0149
6030 Cytochrome P450 2B6 CYP2B6 0.0141
131 Synaptic vesicular amine transporter SLC18A2 0.0131
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0127
465 Calmodulin CALM1 0.0118
713 Sodium-dependent dopamine transporter SLC6A3 0.0103
341 5-hydroxytryptamine 3 receptor HTR3A 0.0102
3923 Cholinesterase BCHE 0.01
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0097
921 Glutamate receptor 2 GRIA2 0.0092
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0091
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0084
528 5-hydroxytryptamine 1E receptor HTR1E 0.0084
3941 Amine oxidase [flavin-containing] A MAOA 0.0077
474 Acetylcholinesterase ACHE 0.0072
6144 Solute carrier family 22 member 2 SLC22A2 0.0063
3939 Amine oxidase [flavin-containing] B MAOB 0.0061
124 Histamine H2 receptor HRH2 0.0061
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0058
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0044
3426 Glutamine synthetase glnA 0.0043
3987 Glutamine synthetase GLUL 0.0043
6432 Transporter snf 0.0042
6859 Protein S100-A4 S100A4 0.0041
694 Matrix protein 2 M 0.0039
6024 Cytochrome P450 1A1 CYP1A1 0.0038
5718 Cytochrome P450 2A6 CYP2A6 0.0036
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0036
380 Cytochrome P450 17A1 CYP17A1 0.0035
427 Substance-P receptor TACR1 0.0034
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0033
6106 Cytochrome P450 2C18 CYP2C18 0.0032
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0031
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.003
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0027
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0027
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0025
866 Large neutral amino acids transporter small subunit 2 SLC7A8 0.0024
20 Prostaglandin G/H synthase 1 PTGS1 0.0024
696 Kappa-type opioid receptor OPRK1 0.0024
6147 Solute carrier family 22 member 3 SLC22A3 0.0024
776 Bile salt export pump ABCB11 0.0023
245 Large neutral amino acids transporter small subunit 1 SLC7A5 0.0023
193 Beta-1 adrenergic receptor ADRB1 0.0023
766 Beta-2 adrenergic receptor ADRB2 0.0022
3947 Xanthine dehydrogenase/oxidase XDH 0.002
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.002
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.002
1656 CYP2B protein CYP2B 0.0019
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0018
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0018
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0018
164 Histamine H4 receptor HRH4 0.0017
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0017
6151 Monocarboxylate transporter 10 SLC16A10 0.0016
904 Glutathione S-transferase P GSTP1 0.0016
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0015
118 Organic cation/carnitine transporter 2 SLC22A5 0.0015
153 Dopamine beta-hydroxylase DBH 0.0014
1360 Sphingomyelin phosphodiesterase SMPD1 0.0014
833 Organic cation/carnitine transporter 1 SLC22A4 0.0014
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0012
3810 Catechol O-methyltransferase COMT 0.0012
1898 Cytochrome P450 1B1 CYP1B1 0.001
1618 High affinity nerve growth factor receptor NTRK1 0.001
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0009
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0007
467 Delta-type opioid receptor OPRD1 0.0006
↑