DT-Web

DB00298 - Dapiprazole


Identification
Name Dapiprazole
Accession Number DB00298 (APRD00902)
Type small molecule
Description Dapiprazole (U.S. trade name Rev-Eyes) is an alpha blocker. It is used to reverse mydriasis after eye examination. [Wikipedia]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 325.4512
Groups approved
Monoisotopic Weight 325.226645889
Pharmacology
Indication Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic (tropicamide) agents used in certain eye examinations.
Mechanism of action Dapiprazole acts through blocking the alpha1-adrenergic receptors in smooth muscle. It produces miosis through an effect on the dilator muscle of the iris and does not have any significant activity on ciliary muscle contraction and, therefore does not induce a significant change in the anterior chamber depth or the thickness of the lens.
Absorption Systemic absorption is negligible.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Oral LD50 is 1189-2100 mg/kg in mice, rats and rabbits.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Tamsulosin Concomitant use of alpha1-adrenergic antagonists, Tamsulosin and Dapiprazole, may result in additive antihypertensive effects. Combination therapy is not recommended.
Food Interactions Not Available

Targets


Alpha-1A adrenergic receptor
Name Alpha-1A adrenergic receptor
Gene Name ADRA1A
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
  • Eltze M: Affinity of the miotic drug, dapiprazole, at alpha 1-adrenoceptor subtypes A, B and D. J Pharm Pharmacol. 1997 Nov;49(11):1091-5. - Pubmed
DTHybrid score 0.4642
Alpha-1D adrenergic receptor
Name Alpha-1D adrenergic receptor
Gene Name ADRA1D
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
DTHybrid score 0.2605
Alpha-1B adrenergic receptor
Name Alpha-1B adrenergic receptor
Gene Name ADRA1B
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
DTHybrid score 0.3623

Predictions


Id Partner name Gene Name Score
318 Alpha-2A adrenergic receptor ADRA2A 0.1404
4119 Cytochrome P450 2D6 CYP2D6 0.0878
502 5-hydroxytryptamine 2A receptor HTR2A 0.0872
4512 Cytochrome P450 3A4 CYP3A4 0.0837
831 D(2) dopamine receptor DRD2 0.0832
629 Alpha-2B adrenergic receptor ADRA2B 0.0782
23 D(1A) dopamine receptor DRD1 0.0757
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0718
378 Alpha-2C adrenergic receptor ADRA2C 0.0641
1588 Multidrug resistance protein 1 ABCB1 0.0635
4200 Cytochrome P450 1A2 CYP1A2 0.0551
590 5-hydroxytryptamine 2C receptor HTR2C 0.0531
320 5-hydroxytryptamine 1A receptor HTR1A 0.0524
492 Histamine H1 receptor HRH1 0.0509
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0485
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0437
193 Beta-1 adrenergic receptor ADRB1 0.0422
432 D(4) dopamine receptor DRD4 0.0414
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0408
766 Beta-2 adrenergic receptor ADRB2 0.0407
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.04
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.04
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0397
713 Sodium-dependent dopamine transporter SLC6A3 0.0397
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0396
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0354
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0347
6016 Cytochrome P450 2C19 CYP2C19 0.0311
6145 Solute carrier family 22 member 1 SLC22A1 0.0304
725 5-hydroxytryptamine 1D receptor HTR1D 0.0301
131 Synaptic vesicular amine transporter SLC18A2 0.0294
638 D(3) dopamine receptor DRD3 0.0286
885 5-hydroxytryptamine 1B receptor HTR1B 0.0252
824 Sodium-dependent serotonin transporter SLC6A4 0.0252
163 D(1B) dopamine receptor DRD5 0.0251
1256 5-hydroxytryptamine 6 receptor HTR6 0.0245
3941 Amine oxidase [flavin-containing] A MAOA 0.0243
4757 Cytochrome P450 2C9 CYP2C9 0.0238
828 Phenylalanine-4-hydroxylase PAH 0.0235
3109 Phenylalanine-4-hydroxylase phhA 0.0235
6138 Multidrug resistance protein 3 ABCB4 0.022
4118 Cytochrome P450 3A5 CYP3A5 0.0195
6144 Solute carrier family 22 member 2 SLC22A2 0.0194
6013 Cytochrome P450 2E1 CYP2E1 0.0193
716 5-hydroxytryptamine 7 receptor HTR7 0.0189
587 Serum albumin ALB 0.0177
6147 Solute carrier family 22 member 3 SLC22A3 0.0162
1517 Beta-3 adrenergic receptor ADRB3 0.0159
436 5-hydroxytryptamine 2B receptor HTR2B 0.0141
6030 Cytochrome P450 2B6 CYP2B6 0.0138
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0124
3876 Aromatic-L-amino-acid decarboxylase DDC 0.012
6107 Cytochrome P450 3A7 CYP3A7 0.0116
528 5-hydroxytryptamine 1E receptor HTR1E 0.0115
118 Organic cation/carnitine transporter 2 SLC22A5 0.0105
1636 Trace amine-associated receptor 1 TAAR1 0.0102
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0099
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0095
341 5-hydroxytryptamine 3 receptor HTR3A 0.0091
3923 Cholinesterase BCHE 0.0091
465 Calmodulin CALM1 0.0089
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0088
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0088
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0086
4924 Cytochrome P450 2C8 CYP2C8 0.0072
6024 Cytochrome P450 1A1 CYP1A1 0.007
233 Potassium channel subfamily K member 2 KCNK2 0.0069
124 Histamine H2 receptor HRH2 0.0067
6151 Monocarboxylate transporter 10 SLC16A10 0.0063
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.006
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.006
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0059
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0059
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0056
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0055
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0054
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0054
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0053
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0052
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0046
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0046
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0045
1656 CYP2B protein CYP2B 0.0044
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0043
6432 Transporter snf 0.004
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0038
3426 Glutamine synthetase glnA 0.0037
3987 Glutamine synthetase GLUL 0.0037
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0037
6859 Protein S100-A4 S100A4 0.0035
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0034
474 Acetylcholinesterase ACHE 0.0032
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0032
4120 NADPH--cytochrome P450 reductase POR 0.003
20 Prostaglandin G/H synthase 1 PTGS1 0.0029
1618 High affinity nerve growth factor receptor NTRK1 0.0029
3947 Xanthine dehydrogenase/oxidase XDH 0.0028
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0028
6106 Cytochrome P450 2C18 CYP2C18 0.0028
833 Organic cation/carnitine transporter 1 SLC22A4 0.0027
776 Bile salt export pump ABCB11 0.0026
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0024
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0022
3939 Amine oxidase [flavin-containing] B MAOB 0.0021
164 Histamine H4 receptor HRH4 0.0019
1374 Natriuretic peptides B NPPB 0.0019
1827 Gap junction alpha-1 protein GJA1 0.0019
1908 Vascular cell adhesion protein 1 VCAM1 0.0019
467 Delta-type opioid receptor OPRD1 0.0018
696 Kappa-type opioid receptor OPRK1 0.0018
194 NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2 0.0016
5718 Cytochrome P450 2A6 CYP2A6 0.0015
183 Vascular endothelial growth factor A VEGFA 0.0014
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
1898 Cytochrome P450 1B1 CYP1B1 0.0011
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