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.
Shanghai Institute of Biochemistry, Chinese Academy of Sciences.
Y C
YC
Du
J H
JH
Wu
X M
XM
Jiang
Y J
YJ
Gu
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)