Glaum S R, Anderson E G
Department of Pharmacology, University of Illinois, Chicago 60612.
Eur J Pharmacol. 1988 Nov 1;156(2):287-90. doi: 10.1016/0014-2999(88)90335-4.
The 5-HT3 receptor antagonists, ICS 205-930 and MDL 72222, displace 47-55% of the specific [3H]serotonin (100 nM) binding to synaptosomal membranes derived from the dorsal, but not ventral, spinal cord of rats with IC50s less than 1.0 nM. Methiothepin (10 microM) increased displacement to 86-94% without shifting these IC50s. Scatchard plots of [3H]5-HT binding in the presence of methiothepin (10 microM) reveal a single population of sites (KD = 11.5 nM, Bmax = 282 fmol mg-1 protein). These results indicate the presence of 5-HT3 binding sites in dorsal spinal cord.
5-羟色胺3（5-HT3）受体拮抗剂ICS 205-930和MDL 72222能够取代47%-55%与大鼠背侧而非腹侧脊髓来源的突触体膜特异性结合的[3H]血清素（100 nM），其半数抑制浓度（IC50）小于1.0 nM。甲硫哒嗪（10 μM）可使取代率提高至86%-94%，而不改变这些IC50值。在存在甲硫哒嗪（10 μM）的情况下，[3H]5-羟色胺结合的Scatchard图显示为单一的位点群体（解离常数KD = 11.5 nM，最大结合容量Bmax = 282 fmol mg-1蛋白质）。这些结果表明在背侧脊髓中存在5-HT3结合位点。
