Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]‐GTP‐γ‐S functional binding assay

@article{Romero1999OpioidPR,
  title={Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective $\mu$/$\kappa$ antagonist in the [35S]‐GTP‐$\gamma$‐S functional binding assay},
  author={D. V. Romero and J. Partilla and Q. X. Zheng and S. Heyliger and Q. Ni and K. Rice and J. Lai and R. Rothman},
  journal={Synapse},
  year={1999},
  volume={34}
}
We utilized the [35S]‐GTP‐γ‐S functional binding assay to determine the selectivity of opioid receptor agonists in guinea pig caudate membranes. The study focused on two opioid agonists used for treating opioid‐dependent patients: methadone and buprenorphine. Selective antagonists were used to generate agonist‐selective conditions: TIPP + nor‐BNI to measure μ receptors, CTAP + nor‐BNI to measure γ receptors and TIPP + CTAP to measure κ receptors. The assay was first validated with opioid… Expand
Comparison of the in vitro efficacy of μ, δ, κ and ORL1 receptor agonists and non-selective opioid agonists in dog brain membranes
Morphine and related opioid agonists are frequently used in dogs for their analgesic properties, their sedative effects and as adjuncts to anesthesia. Such compounds may be effective through aExpand
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The binding of norBUP to opioid and nociceptin/orphanin FQ (ORL1) receptors, and its effects on [(35)S]guanosine-5'-O-(gamma-thio)triphosphate ([(35]S]GTP gamma S) binding mediated by opioid or ORL1 receptors are described and highlighted. Expand
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Evidence regarding the activation of μ-opioid receptor (MOR)-related G proteins by iboga alkaloids is replicated and extended to suggest a novel mechanism of action, and further justify the search for alternative targets of ibogamine skeleton compounds. Expand
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