Orphanin FQ: Receptor binding and analog structure activity relationships in rat brain Article

Dooley, CT, Houghten, RA. (1996). Orphanin FQ: Receptor binding and analog structure activity relationships in rat brain . LIFE SCIENCES, 59(1), 10.1016/0024-3205(96)00261-5

cited authors

  • Dooley, CT; Houghten, RA

abstract

  • A tritiated form of orphanin FQ (a heptadecapeptide also known as Nociceptin) has been prepared. This radioligand (33 Ci/mmole) was used to develop a radioreceptor assay using rat brain homogenates. Binding was observed to be saturable, and analyses of the binding data indicate the presence of a single binding site with a dissociation constant of 5 ± 1.1 nM and Bmax of 535 ± 85 fmoles/mg protein. Thirty-four analogues of orphanin FQ, including a complete alanine 'scan' of orphanin FQ, and truncation analogues from both the N- and C- terminals were synthesized and tested. The data obtained indicate that the N-terminus plays a more critical role in binding than the C-terminus and that residues 1, 2, 4, and 8 are essential for binding.

publication date

  • May 31, 1996

published in

Digital Object Identifier (DOI)

volume

  • 59

issue

  • 1