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Can I read Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]-GTP-γ-S functional binding assay on EtoBox?
Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]-GTP-γ-S functional binding assay by Dana V. Romero; John S. Partilla; Qaio-Xi Zheng; Simone O. Heyliger; Qing Ni; Kenner C. Rice; Josephine Lai; Richard B. Rothman is a Neuroscience article available to read on EtoBox.
What is Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]-GTP-γ-S functional binding assay about?
We utilized the [ 35 S]-GTP-␥-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 ϩ nor-BNI to measure μ receptors, CTAP ϩ nor-BNI to measure ␥ receptors and TIPP ϩ CTAP to measure receptors. The assay was first validated with opioid agonists of known subtype specificity (DAMGO for μ, SNC80 for ␦, and U69,593 for receptors). Methadone-stimulated [ 35 S]-GTP-␥-S binding was μ-specific and less potent and efficacious than etorphine (K d ϭ 1,537 nM vs. K d ϭ 7.8 nM). Buprenorphine failed to stimulate [ 35 S]-GTP-␥-S binding but inhibited agonist-stimulated [ 35 S]-GTP-␥-S binding. The antagonist-K i values (nM) of buprenorphine at μ, ␦, and receptors were 0.088 nM, 1.15 nM, and 0.072 nM, respectively. The antagonist-K i values (nM) of naloxone at μ, ␦, and receptors were 1.39 nM, 25.0 nM, and 11.4 nM, respectively. Autoradiographic studies showed that buprenorphine failed to stimulate [ 35 S]-GTP-␥-S binding in caudatelevel rat br
Who reads Opioid peptide receptor studies. 12. Buprenorphine is a potent and selective μ/κ antagonist in the [35S]-GTP-γ-S functional binding assay?
It is typically read by researchers, students, and practitioners in Neuroscience.
- Author
- Dana V. Romero; John S. Partilla; Qaio-Xi Zheng; Simone O. Heyliger; Qing Ni; Kenner C. Rice; Josephine Lai; Richard B. Rothman
- Publisher
- John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0887-4476)
- Published
- 1999
- Language
- EN
- Field
- Neuroscience (Life Sciences)