Identification of 5-HT3 binding sites in rat spinal cord synaptosomal membranes.
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.
Glaum
S R
SR
Department of Pharmacology, University of Illinois, Chicago 60612.
Anderson
E G
EG
D001665:Binding Sites; D002462:Cell Membrane / Q000378:metabolism; D007211:Indoles / Q000494:pharmacology; D008719:Methiothepin / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000145:classification / Q000187:drug effects / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists; D013116:Spinal Cord / Q000378:metabolism*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism; D014326:Tropanes / Q000494:pharmacology; D000077526:Tropisetron
D007211:Indoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014326:Tropanes; D012701:Serotonin; D008719:Methiothepin; D000077526:Tropisetron; C042253:bemesetron