Comparison of [3H]YM060 binding to native and cloned rat 5-HT3 receptors.
We characterized [3H]YM060 ([methyl-3H]-(-)-(R)-5-[(methyl-1H- indol-3-yl)carbonyl]-4,5,6,7-tetrahydro-1H-benzimidazole monohydrochloride) binding in membrane homogenates prepared from three different rat tissues (cerebral cortex, ileum and colon), and compared the binding characteristics between the native and cloned rat 5-HT3 receptors. The dissociation constant (Kd) of [3H]YM060 was similar in all membranes. In competition studies, the affinity of 5-HT3 receptor agonists and antagonists was similar between the native and the cloned rat 5-HT3 receptors. In conclusion, intra-species difference of 5-HT3 receptor was not observed in rats and pharmacological properties of the cloned rat 5-HT3 receptor were nearly identical to that of the native rat 5-HT3 receptor.
Akuzawa
S
S
Department of Internal Medicine, University of Tsukuba, Ibaraki, Japan.
Miyake
A
A
Miyata
K
K
Fukutomi
H
H
D000818:Animals; D001562:Benzimidazoles / Q000378:metabolism*; D003001:Cloning, Molecular; D066298:In Vitro Techniques; D008297:Male; D011485:Protein Binding; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D011985:Receptors, Serotonin / Q000235:genetics / Q000378:metabolism*; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists / Q000378:metabolism*
D001562:Benzimidazoles; D011985:Receptors, Serotonin; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists; C071315:ramosetron