[3H]L-694,247 labels the 5-HT1D beta receptor in pig caudate membranes.
This study, carried out in pig caudate membranes, characterises the radioligand binding site labelled with [3H]L-694,247 (2-[5-[3-(4-methylsulphonylamino)benzyl-1,2,4-oxadiazol-5-yl ]-1H-indole-3 - yl]ethylamine). The affinities of 27 standard compounds are consistent with binding to a 5-HT1D recognition site. In addition the results indicate that, under the assay conditions described, [3H]L-694,247 specifically labels the 5-HT1D beta recognition site since ketanserin and ritanserin display a low affinity consistent with their activities at this subtype of the 5-HT1D receptor.
Heald
A
A
Merck Sharp Research Laboratory, Neuroscience Research Centre, Harlow, Essex, UK.
Stanton
J A
JA
Osborne
S A
SA
Middlemiss
D N
DN
Beer
M S
MS
D000818:Animals; D001667:Binding, Competitive; D002421:Caudate Nucleus / Q000187:drug effects / Q000378:metabolism*; D005629:Frozen Sections; D010069:Oxadiazoles / Q000378:metabolism* / Q000494:pharmacology; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D017366:Serotonin Receptor Agonists / Q000378:metabolism* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013552:Swine; D014021:Tissue Preservation; D014363:Tryptamines / Q000378:metabolism* / Q000494:pharmacology
D010069:Oxadiazoles; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; C085632:L 694247