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Prolonged opioid exposure increases the expression of cholecystokinin (CCK) and its receptors in the central nervous system (CNS), where CCK may attenuate the antinociceptive effects of opioids. The complex interactions between opioid and CCK may play a role in the development of opioid tolerance. We designed and synthesized cyclic disulfide peptides and determined their agonist properties at opioid...
Xu, H., Y-F. Lu, J. S. Partilla, J. Pinto, S. N. Calderon, D. Matecka, K. C. Rice, J. Lai, F. Porreca, S. Ananthan and R. B. Rothman. Opioid peptide receptor studies. 8. One of the mouse brain δ NCX binding sites is similar to the cloned moused opioid δ receptor: further evidence for heterogeneity of δ opioid receptors. Peptides 19(2) 343-350, 1998.-Quantitative ligand binding studies...
Quantitative binding studies resolved two high-affinity [ 3 H][d-Ala 2 ,d-Leu 5 ]enkephalin binding sites in rat brain membranes depleted of μ binding sites by pretreatment with the irreversible agent BIT.-- The two binding sites had lower (δ ncx-2 , Ki = 96.6 nM) and higher (δ ncx-1 , Ki = 1.55 nM) affinity for DPDPE...
Four isomers of the Somatostatin analogue H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH 2 (CTAP) were made with β-MePhe in position 1 and assayed for opioid binding in rat brain, biological activity in MVD and GPI bioassays, and antinociception in mouse warm-water tail flick assays. These analogues displayed varying potencies and biological activities including: simultaneous δ receptor agonism/μ...
Our laboratory was among the first to propose the existence of δ receptor subtypes: a δ site throught to be associated with a μ--δ-opinoid receptor complex termed the δ cx binding site and δ site not associated with the μ--δ-opinoid receptor complex, termed the δ ncx site. In previous studies, we assayed the δ cx site with [ 3 H][d-Ala 2 ...
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