DT-Web

DB01548 - Diprenorphine


Identification
Name Diprenorphine
Accession Number DB01548
Type small molecule
Description A narcotic antagonist similar in action to naloxone. It is used to remobilize animals after etorphine neuroleptanalgesia and is considered a specific antagonist to etorphine. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 425.5604
Groups illicit
Monoisotopic Weight 425.256608613
Pharmacology
Indication Diprenorphine is used to reverse the effects of the super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals in veterinary medicine. Not used in humans.
Mechanism of action Diprenorphine binds approximately equally to the three subtypes of opioid receptorsand antagonizes them.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Mu-type opioid receptor
Name Mu-type opioid receptor
Gene Name OPRM1
Pharmacological action yes
Actions antagonist
References
  • Leung K: [6-O-methyl-11C]Diprenorphine - Pubmed
DTHybrid score 1.1162
Delta-type opioid receptor
Name Delta-type opioid receptor
Gene Name OPRD1
Pharmacological action yes
Actions antagonist
References
  • Willoch F, Tolle TR, Wester HJ, Munz F, Petzold A, Schwaiger M, Conrad B, Bartenstein P: Central pain after pontine infarction is associated with changes in opioid receptor binding: a PET study with 11C-diprenorphine. AJNR Am J Neuroradiol. 1999 Apr;20(4):686-90. - Pubmed
  • Jones AK, Kitchen ND, Watabe H, Cunningham VJ, Jones T, Luthra SK, Thomas DG: Measurement of changes in opioid receptor binding in vivo during trigeminal neuralgic pain using [11C] diprenorphine and positron emission tomography. J Cereb Blood Flow Metab. 1999 Jul;19(7):803-8. - Pubmed
  • Kampa M, Hatzoglou A, Notas G, Niniraki M, Kouroumalis E, Castanas E: Opioids are non-competitive inhibitors of nitric oxide synthase in T47D human breast cancer cells. Cell Death Differ. 2001 Sep;8(9):943-52. - Pubmed
  • Marie N, Lecoq I, Jauzac P, Allouche S: Differential sorting of human delta-opioid receptors after internalization by peptide and alkaloid agonists. J Biol Chem. 2003 Jun 20;278(25):22795-804. Epub 2003 Apr 2. - Pubmed
  • Webster JM, Bentley MT, Wojcikiewicz RJ: N,N,N',N'-tetrakis(2-pyridylmethyl)ethylenediamine inhibits ligand binding to certain G protein-coupled receptors. Eur J Pharmacol. 2003 Aug 1;474(1):1-5. - Pubmed
  • Leung K: [6-O-methyl-11C]Diprenorphine - Pubmed
DTHybrid score 0.9509
Kappa-type opioid receptor
Name Kappa-type opioid receptor
Gene Name OPRK1
Pharmacological action unknown
Actions antagonist
References
  • Leung K: [6-O-methyl-11C]Diprenorphine - Pubmed
DTHybrid score 0.9267
Tripartite motif-containing protein 13
Name Tripartite motif-containing protein 13
Gene Name TRIM13
Pharmacological action unknown
Actions Not Available
References
  • Law PY, Hom DS, Loh HH: Multiple affinity states of opiate receptor in neuroblastoma x glioma NG108-15 hybrid cells. Opiate agonist association rate is a function of receptor occupancy. J Biol Chem. 1985 Mar 25;260(6):3561-9. - Pubmed
  • Pfeiffer A, Herz A: Discrimination of three opiate receptor binding sites with the use of a computerized curve-fitting technique. Mol Pharmacol. 1982 Mar;21(2):266-71. - Pubmed
  • Chang KJ, Hazum E, Cuatrecasas P: Novel opiate binding sites selective for benzomorphan drugs. Proc Natl Acad Sci U S A. 1981 Jul;78(7):4141-5. - Pubmed
  • Pfeiffer A, Herz A: Enhancement of delta- but not mu-opiate agonist binding by calcium. Naunyn Schmiedebergs Arch Pharmacol. 1982 May;319(2):147-53. - Pubmed
  • Cvejic S, Trapaidze N, Cyr C, Devi LA: Thr353, located within the COOH-terminal tail of the delta opiate receptor, is involved in receptor down-regulation. J Biol Chem. 1996 Feb 23;271(8):4073-6. - Pubmed
DTHybrid score 0.4959

Predictions


Id Partner name Gene Name Score
1262 Corticotropin-lipotropin POMC 0.2585
4137 Nociceptin receptor OPRL1 0.1471
4512 Cytochrome P450 3A4 CYP3A4 0.1082
4119 Cytochrome P450 2D6 CYP2D6 0.1049
6107 Cytochrome P450 3A7 CYP3A7 0.0588
1588 Multidrug resistance protein 1 ABCB1 0.0474
4118 Cytochrome P450 3A5 CYP3A5 0.0443
4924 Cytochrome P450 2C8 CYP2C8 0.0385
319 Opioid receptor, sigma 1 OPRS1 0.0343
4757 Cytochrome P450 2C9 CYP2C9 0.0338
174 Sigma 1-type opioid receptor SIGMAR1 0.0337
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0291
6180 UDP-glucuronosyltransferase 2B4 UGT2B4 0.0287
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0278
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0247
6030 Cytochrome P450 2B6 CYP2B6 0.024
824 Sodium-dependent serotonin transporter SLC6A4 0.0188
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0186
5838 Transient receptor potential cation channel subfamily V member 3 TRPV3 0.0176
2162 Transient receptor potential cation channel subfamily M member 8 TRPM8 0.0176
1944 Transient receptor potential cation channel subfamily A member 1 TRPA1 0.0176
6016 Cytochrome P450 2C19 CYP2C19 0.0168
1291 cAMP response element-binding protein CREB1 0.0166
341 5-hydroxytryptamine 3 receptor HTR3A 0.0164
4210 Toll-like receptor 4 TLR4 0.015
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.014
587 Serum albumin ALB 0.0137
392 Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A 0.0136
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0127
4200 Cytochrome P450 1A2 CYP1A2 0.0121
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0118
590 5-hydroxytryptamine 2C receptor HTR2C 0.0113
6106 Cytochrome P450 2C18 CYP2C18 0.0107
20 Prostaglandin G/H synthase 1 PTGS1 0.01
465 Calmodulin CALM1 0.0097
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0094
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.009
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0088
6145 Solute carrier family 22 member 1 SLC22A1 0.0084
136 Estrogen receptor ESR1 0.0082
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0079
3811 Cytochrome P450 19A1 CYP19A1 0.0079
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0065
4120 NADPH--cytochrome P450 reductase POR 0.006
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0058
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0055
5718 Cytochrome P450 2A6 CYP2A6 0.0053
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0051
318 Alpha-2A adrenergic receptor ADRA2A 0.0048
502 5-hydroxytryptamine 2A receptor HTR2A 0.0046
439 Glutamate [NMDA] receptor subunit epsilon-4 GRIN2D 0.0045
492 Histamine H1 receptor HRH1 0.0045
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0044
505 Glutamate [NMDA] receptor subunit epsilon-3 GRIN2C 0.0044
320 5-hydroxytryptamine 1A receptor HTR1A 0.0043
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0041
401 Glutamate [NMDA] receptor subunit zeta-1 GRIN1 0.0039
837 Glutamate [NMDA] receptor subunit epsilon-1 GRIN2A 0.0039
94 5-hydroxytryptamine 4 receptor HTR4 0.0035
6013 Cytochrome P450 2E1 CYP2E1 0.0035
1618 High affinity nerve growth factor receptor NTRK1 0.0034
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0033
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0033
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0033
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0027
885 5-hydroxytryptamine 1B receptor HTR1B 0.0025
789 Alpha-1D adrenergic receptor ADRA1D 0.0023
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0022
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0021
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0019
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0018
556 Alpha-1A adrenergic receptor ADRA1A 0.0018
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