[3H]neurotensin(8-13) binds in human brain to the same sites as does [3H]neurotensin but with higher affinity.
The binding of [3H]neurotensin(8-13) to membranes from human frontal cortex at 0 degree C was time dependent, specific, saturable, and reversible. Saturation isotherms provided an equilibrium dissociation constant (KD) of 0.52 nM, and the maximal number of binding sites (Bmax) was 3.5 pmol/g original wet weight of tissue. Scatchard analysis yielded a straight line, and the Hill coefficient was equal to 1, a result indicating that [3H]neurotensin(8-13) bound to single, noncoopertive sites. The KD values of several analogs of neurotensin determined in competition with [3H]neurotensin(8-13) were similar to those previously determined in competition with [3H]neurotensin. The regional distribution of binding sites for [3H]neurotensin(8-13) was also similar to that for [3H]neurotensin. These results suggest that [3H]neurotensin(8-13) binds to the same sites as [3H]neurotensin and that [3H]neurotensin(8-13) has a higher affinity than [3H]neurotensin for these sites in human brain.
Kanba
K S
KS
Department of Psychiatry, Mayo Clinic and Foundation, Rochester, Minnesota.
Kanba
S
S
Nelson
A
A
Okazaki
H
H
Richelson
E
E
D000368:Aged; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D005260:Female; D005625:Frontal Lobe / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D009496:Neurotensin / Q000378:metabolism*; D010446:Peptide Fragments / Q000378:metabolism*; D018028:Receptors, Neurotensin; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D014018:Tissue Distribution; D014316:Tritium
D010446:Peptide Fragments; D018028:Receptors, Neurotensin; D017981:Receptors, Neurotransmitter; D014316:Tritium; D009496:Neurotensin; C054381:neurotensin (8-13)