Improvements on a chemically contiguous hapten for a vaccine to address fentanyl-contaminated heroin.
Active immunization
Antibody
Chemical biology
Fentanyl
Heroin
Immunopharmacotherapy
Medicinal chemistry
Opioid vaccine
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 07 2021
01 07 2021
Historique:
received:
23
04
2021
revised:
13
05
2021
accepted:
18
05
2021
pubmed:
26
5
2021
medline:
9
11
2021
entrez:
25
5
2021
Statut:
ppublish
Résumé
Unintentional overdose deaths related to opioids and psychostimulants have increased in prevalence due to the adulteration of these drugs with fentanyl. Synergistic effects between illicit compounds and fentanyl cause aggravated respiratory depression, leading to inadvertent fatalities. Traditional small-molecule therapies implemented in the expanding opioid epidemic present numerous problems since they interact with the same opioid receptors in the brain as the abused drugs. In this study, we report an optimized dual hapten for use as an immunopharmacotherapeutic tool in order to develop antibodies capable of binding to fentanyl-contaminated heroin in the periphery, thus impeding the drugs' psychoactive effects on the central nervous system. This vaccine produced antibodies with nanomolar affinities and effectively blocked opioid analgesic effects elicited by adulterated heroin. These findings provide further insight into the development of chemically contiguous haptens for broad-spectrum immunopharmacotherapies against opioid use disorders.
Identifiants
pubmed: 34034147
pii: S0968-0896(21)00233-9
doi: 10.1016/j.bmc.2021.116225
pii:
doi:
Substances chimiques
Haptens
0
Vaccines
0
Heroin
70D95007SX
Fentanyl
UF599785JZ
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
116225Informations de copyright
Copyright © 2021 Elsevier Ltd. All rights reserved.