Drug Information

Drug (ID: DG01082) and It's Reported Resistant Information

• Name: Dezocine
• Synonyms: DEZOCINE; Dalgan; 53648-55-8; Dezocina; Dezocinum; Dezocinum [INN-Latin]; Dezocina [INN-Spanish]; UNII-VHX8K5SV4X; Wy-16225; VHX8K5SV4X; CHEMBL1685; CHEBI:4474; (-)-13beta-Amino-5,6,7,8,9,10,11alpha,12-octahydro-5alpha-methyl-5,11-methanobenzocyclodecen-3-ol; Wy-16,225; (1R,9S,15S)-15-amino-1-methyltricyclo[7.5.1.02,7]pentadeca-2(7),3,5-trien-4-ol; Dezocine [USAN:INN]; Docozine; Dozocine; Dezocine (USAN); Dalgan (TN); WY 16225; WY 16,225; SCHEMBL3072; DTXSID2022911; (5R,11S,13S)-13-amino-5-methyl-5,6,7,8,9,10,11,12-octahydro-5,11-methanobenzo[10]annulen-3-ol; BDBM50276568; AKOS016014025; DB01209; C08010; D00838; Q1109018; (1R,9S,15S)-15-amino-1-methyltricyclo[7.5.1.0^{2,7}]pentadeca-2,4,6-trien-4-ol; 13-Amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecenol; (5R,11S,13S)-13-amino-5-methyl-5,6,7,8,9,10,11,12-octahydro-5,11-methanobenzocyclodecen-3-ol; 5,11-Methanobenzocyclodecen-3-ol, 13-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-, (5alpha,11alpha,13S*)-, (-)-
• Indication:
  In total 1 Indication(s)
  Pain [ICD-11: MG30]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
  Pain [ICD-11: MG30]; [1]
• Target: Opioid receptor kappa (OPRK1); OPRK_HUMAN; [1]
• Formula: C16H23NO
• IsoSMILES: C[C@]12CCCCC[C@H]([C@@H]1N)CC3=C2C=C(C=C3)O
• InChI: 1S/C16H23NO/c1-16-8-4-2-3-5-12(15(16)17)9-11-6-7-13(18)10-14(11)16/h6-7,10,12,15,18H,2-5,8-9,17H2,1H3/t12-,15-,16+/m0/s1
• InChIKey: VTMVHDZWSFQSQP-VBNZEHGJSA-N
• PubChem CID: 3033053
• ChEBI ID: CHEBI:4474
• TTD Drug ID: D0P6VV
• DrugBank ID: DB01209

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-21: Symptoms/clinical signs/unclassified clinical findings

Pain [ICD-11: MG30]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: hsa-miR-124-3p [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Pain [ICD-11: MG30.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• Experiment for Molecule Alteration: Western blot analysis; Quantitative reverse-transcription PCR assay
• Mechanism Description: miR-124-3p alleviates the dezocine tolerance against pain by regulating TRAF6 in a rat model. miR-124-3p expression was highly downregulated in a dezocine-resistant model. miR-124-3p overexpression could alleviate dezocine tolerance in rats. TRAF6 expression was significantly upregulated in a dezocine-resistant model. miR-124-3p targeted TRAF6 and TRAF6 was negatively modulated by miR-124-3p. In addition, overexpression of TRAF6 could reverse the inhibitory effects of miR-124-3p on dezocine tolerance. Overexpression of miR-124-3p alleviates dezocine tolerance against pain via regulating TRAF6 in a rat model, providing a possible solution to address dezocine tolerance in clinical.

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: TNF receptor-associated factor 6 (TRAF6) [1]

• Molecule Alteration: Expression; Up-regulation
• Resistant Disease: Pain [ICD-11: MG30.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• Experiment for Molecule Alteration: Western blot analysis; Quantitative reverse-transcription PCR assay
• Mechanism Description: miR-124-3p alleviates the dezocine tolerance against pain by regulating TRAF6 in a rat model. miR-124-3p expression was highly downregulated in a dezocine-resistant model. miR-124-3p overexpression could alleviate dezocine tolerance in rats. TRAF6 expression was significantly upregulated in a dezocine-resistant model. miR-124-3p targeted TRAF6 and TRAF6 was negatively modulated by miR-124-3p. In addition, overexpression of TRAF6 could reverse the inhibitory effects of miR-124-3p on dezocine tolerance. Overexpression of miR-124-3p alleviates dezocine tolerance against pain via regulating TRAF6 in a rat model, providing a possible solution to address dezocine tolerance in clinical.

References

• Ref 1: MiR-124-3p alleviates the dezocine tolerance against pain by regulating TRAF6 in a rat model .Neuroreport. 2021 Jan 6;32(1):44-51. doi: 10.1097/WNR.0000000000001559. 10.1097/WNR.0000000000001559