DT-Web

DB01209 - Dezocine


Identification
Name Dezocine
Accession Number DB01209 (APRD00912)
Type small molecule
Description Dezocine is a partial opiate drug and is used for pain management. Dezocine is a very effective alternative to fentanyl when administered during outpatient laparoscopy, although is associated with an increased incidence of postoperative nausea.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 245.3599
Groups approved
Monoisotopic Weight 245.177964363
Pharmacology
Indication Indicated in the treatment of moderate to severe pain.
Mechanism of action Dezocine is a opioid analgesic drug of mixed agonist-antagonist type. It binds with stereospecific receptors at many sites within the central nervous system (CNS) to alter processes affecting both the perception of pain and the emotional response to pain. At least 2 of these types of receptors (mu and kappa) mediate analgesia. Mu receptors are widely distributed throughout the CNS, especially in the limbic system (frontal cortex, temporal cortex, amygdala, and hippocampus), thalamus, striatum, hypothalamus, and midbrain as well as laminae I, II, IV, and V of the dorsal horn in the spinal cord. Kappa receptors are localized primarily in the spinal cord and in the cerebral cortex.
Absorption Rapid and complete following intramuscular administration.
Protein binding Not Available
Biotransformation Hepatic, via conjugation (glucuronidation).
Route of elimination Not Available
Toxicity Symptoms of overdose include cold and clammy skin, confusion, nervousness, or severe restlessness, convulsions (seizures), severe dizziness, severe drowsiness, low blood pressure, pinpoint pupils of eyes, slow heartbeat, slow or troubled breathing and severe weakness.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Alvimopan Increases levels by receptor binding competition. Discontinue opioid administration at least 7 days prior to administrating Alvimopan.
Triprolidine The CNS depressants, Triprolidine and Dezocine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Food Interactions Not Available

Targets


Mu-type opioid receptor
Name Mu-type opioid receptor
Gene Name OPRM1
Pharmacological action yes
Actions agonist
References
  • Picker MJ: Discriminative stimulus effects of the mixed-opioid agonist/antagonist dezocine: cross-substitution by mu and delta opioid agonists. J Pharmacol Exp Ther. 1997 Dec;283(3):1009-17. - Pubmed
  • Barrett AC, Cook CD, Terner JM, Craft RM, Picker MJ: Importance of sex and relative efficacy at the mu opioid receptor in the development of tolerance and cross-tolerance to the antinociceptive effects of opioids. Psychopharmacology (Berl). 2001 Nov;158(2):154-64. - Pubmed
  • Cook CD, Barrett AC, Roach EL, Bowman JR, Picker MJ: Sex-related differences in the antinociceptive effects of opioids: importance of rat genotype, nociceptive stimulus intensity, and efficacy at the mu opioid receptor. Psychopharmacology (Berl). 2000 Jul;150(4):430-42. - Pubmed
  • Gharagozlou P, Demirci H, David Clark J, Lameh J: Activity of opioid ligands in cells expressing cloned mu opioid receptors. BMC Pharmacol. 2003 Jan 4;3:1. Epub 2003 Jan 4. - Pubmed
  • Morgan D, Cook CD, Smith MA, Picker MJ: An examination of the interactions between the antinociceptive effects of morphine and various mu-opioids: the role of intrinsic efficacy and stimulus intensity. Anesth Analg. 1999 Feb;88(2):407-13. - Pubmed
  • Jacobs AM, Youngblood F: Opioid receptor affinity for agonist-antagonist analgesics. J Am Podiatr Med Assoc. 1992 Oct;82(10):520-4. - Pubmed
DTHybrid score 0.6865
Kappa-type opioid receptor
Name Kappa-type opioid receptor
Gene Name OPRK1
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
  • Gharagozlou P, Hashemi E, DeLorey TM, Clark JD, Lameh J: Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.5429

Predictions


Id Partner name Gene Name Score
467 Delta-type opioid receptor OPRD1 0.4461
1716 Tripartite motif-containing protein 13 TRIM13 0.0737
4119 Cytochrome P450 2D6 CYP2D6 0.0706
4512 Cytochrome P450 3A4 CYP3A4 0.0697
1262 Corticotropin-lipotropin POMC 0.0533
6107 Cytochrome P450 3A7 CYP3A7 0.0414
174 Sigma 1-type opioid receptor SIGMAR1 0.0337
1588 Multidrug resistance protein 1 ABCB1 0.0307
4118 Cytochrome P450 3A5 CYP3A5 0.0304
4137 Nociceptin receptor OPRL1 0.025
4924 Cytochrome P450 2C8 CYP2C8 0.0247
4757 Cytochrome P450 2C9 CYP2C9 0.0223
319 Opioid receptor, sigma 1 OPRS1 0.022
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0187
6180 UDP-glucuronosyltransferase 2B4 UGT2B4 0.0184
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0179
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
6030 Cytochrome P450 2B6 CYP2B6 0.0167
6022 UDP-glucuronosyltransferase 1-1 UGT1A1 0.0159
341 5-hydroxytryptamine 3 receptor HTR3A 0.0128
824 Sodium-dependent serotonin transporter SLC6A4 0.0118
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0116
6016 Cytochrome P450 2C19 CYP2C19 0.0107
1291 cAMP response element-binding protein CREB1 0.0107
587 Serum albumin ALB 0.0105
4210 Toll-like receptor 4 TLR4 0.0096
392 Voltage-dependent P/Q-type calcium channel subunit alpha-1A CACNA1A 0.0087
590 5-hydroxytryptamine 2C receptor HTR2C 0.0084
4200 Cytochrome P450 1A2 CYP1A2 0.0084
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0082
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0081
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0078
6181 UDP-glucuronosyltransferase 1-8 UGT1A8 0.0076
6078 Neuronal acetylcholine receptor subunit beta-4 CHRNB4 0.0065
20 Prostaglandin G/H synthase 1 PTGS1 0.0064
465 Calmodulin CALM1 0.0063
6106 Cytochrome P450 2C18 CYP2C18 0.006
4120 NADPH--cytochrome P450 reductase POR 0.006
3811 Cytochrome P450 19A1 CYP19A1 0.0058
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0058
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0058
6079 Neuronal acetylcholine receptor subunit alpha-3 CHRNA3 0.0058
6145 Solute carrier family 22 member 1 SLC22A1 0.0054
136 Estrogen receptor ESR1 0.0053
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0051
439 Glutamate [NMDA] receptor subunit epsilon-4 GRIN2D 0.0045
505 Glutamate [NMDA] receptor subunit epsilon-3 GRIN2C 0.0044
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
318 Alpha-2A adrenergic receptor ADRA2A 0.0038
502 5-hydroxytryptamine 2A receptor HTR2A 0.0037
492 Histamine H1 receptor HRH1 0.0035
94 5-hydroxytryptamine 4 receptor HTR4 0.0035
5718 Cytochrome P450 2A6 CYP2A6 0.0034
320 5-hydroxytryptamine 1A receptor HTR1A 0.0033
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0033
6013 Cytochrome P450 2E1 CYP2E1 0.0026
885 5-hydroxytryptamine 1B receptor HTR1B 0.0025
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.0025
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0022
1618 High affinity nerve growth factor receptor NTRK1 0.0017
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0016
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0016
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0016
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0013
789 Alpha-1D adrenergic receptor ADRA1D 0.0011
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0011
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0011
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0009
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0009
556 Alpha-1A adrenergic receptor ADRA1A 0.0009
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