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The basal (constitutive) activity of G protein‐coupled receptors allows for the measurement of inverse agonist activity. Some competitive antagonists turn into inverse agonists under conditions where receptors are constitutively active. In contrast, neutral antagonists have no inverse agonist activity, and they block both agonist and inverse agonist activity. The μ‐opioid receptor (MOR) demonstrates...
Recent evidence indicates that agonist ligands of G protein coupled receptors (GPCR) can activate different signaling systems. Such “agonist-directed” signaling also occurs with opioid receptors. Previous work from our laboratory showed that chronic morphine, but not DAMGO, up-regulates the expression of Gα12 and that both morphine and DAMGO decreased Gαi3 expression in CHO cells expressing the cloned...
Based on non-competitive binding interactions we suggested that μ and δ receptors associate as a μ/δ receptor complex in rat brain. We hypothesized that the same non-competitive binding interactions observed in rat brain will be seen in CHO cells that co-express μ and δ receptors, but not in cells that express just μ or δ receptors. We used CHO cells expressing the cloned human μ receptor, cloned...
Previous experiments conducted in this laboratory showed that intracerebroventricular (i.c.v.) administration of IgG antibodies directed against selected neuropeptides changed the density of CNS receptors, suggesting that neuropeptides in the cerebrospinal fluid can perform a regulatory role. To further test this hypothesis, we administered anti-CART peptide (the peptide product of cocaine amphetamine...
Prior work in our laboratory has identified putative subtypes of δ (δ cx-1 , δ cx-2 , δ ncx-1 , δ ncx-2 ) and κ 2 (κ 2a and κ 2b ) receptors. Previous studies showed that chronic (three day) i.c.v. administration of antisense oligodeoxynucleotide to the cloned δ...
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