IUPHAR themed review: Opioid efficacy, bias, and selectivity.

ABSTRACT: Drugs acting at the opioid receptor family are clinically used to treat chronic and acute pain, though they represent the second line of treatment behind GABA analogs, antidepressants and SSRI's. Within the opioid family mu and kappa opioid receptor are commonly targeted. However, activation of the mu opioid receptor has side effects of constipation, tolerance, dependence, euphoria, and respiratory depression; activation of the kappa opioid receptor leads to dysphoria and sedation. The side effects of mu opioid receptor activation have led to mu receptor drugs being widely abused with great overdose risk. For these reasons, newer safer opioid analgesics are in high demand. For many years a focus within the opioid field was finding drugs that activated the G protein pathway at mu opioid rec

SUBMITTER: Ramos-Gonzalez N 

PROVIDER: S-EPMC10713092 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature