Characterization of binding sites of a memory-enhancing peptide AVP(4-8) in rat cortical synaptosomal membranes.
The pentapeptide pGlu-Asn-Cyt-Pro-Arg [AVP(4-8), termed ZNC(C)PR in this article] has been found as a metabolite of arginine-vasopressin (AVP) in rat brain and has been shown to have potent memory-enhancing activity and to yield a series of biochemical events in brain tissues. [35S]ZNC(C)PR was chemically synthesized with high specific activity (232 Ci/mmol), and specific binding sites for ZNC(C)PR were located in synaptosomal membrane preparations of rat brain. We identified a specific binding site for ZNC(C)PR with a Kd of 3.12 nM and Bmax of 31 fmol/mg protein in anterior cortical synaptosomal membranes in the presence of 5 mM Ni2+. A comparison of synthetic analogues of ZNC(C)PR competing with [35S]ZNC(C)PR for binding to anterior cortical receptor are presented. ZDC(C)PR, a 2-aspartyl substitute of the 2-asparaginyl residue in ZNC(C)PR, had the most potent competition, but AVP did not show significant ability to compete for the receptor with ZNC(C)PR.
Du
Y C
YC
Shanghai Institute of Biochemistry, Chinese Academy of Sciences.
Wu
J H
JH
Jiang
X M
XM
Gu
Y J
YJ
D000595:Amino Acid Sequence; D000818:Animals; D001127:Arginine Vasopressin / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D001362:Avoidance Learning / Q000187:drug effects; D001665:Binding Sites; D002540:Cerebral Cortex / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008568:Memory / Q000187:drug effects*; D008969:Molecular Sequence Data; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013574:Synaptosomes / Q000378:metabolism*
D010446:Peptide Fragments; D001127:Arginine Vasopressin; C072508:argipressin (4-8)