We have stably expressed the rat 5-HT 6 receptor in HEK293 cells at a density of >2 pmol/mg protein, as determined in equilibrium binding studies with ( 3 H)-LSD and ( 3 H)-5-HT and compared the affinity of a range of compounds in competition binding experiments with either ( 3 H)-LSD or ( 3 H)-5-HT as radioligand. A variety of tryptamine derivatives were tested and showed a significantly higher affinity when the 5-HT 6 receptor was labelled with ( 3 H)-5-HT, whereas ergoline compounds and several antagonists had higher affinities when ( 3 H)-LSD was used as radioligand. Subsequently we examined the ability of LSD, 5-HT and a number of tryptamine derivatives to stimulate cAMP accumulation in order to determine their agonist potency and efficacy. We observed the following rank order of potency: LSD > ω- N -methyl-5-HT ≈ bufotenine ≈ 5-methoxytryptamine > 5-HT > 2-methyl-5-HT ≈ 5-benzyloxytryptamine ≈ tryptamine > 5-carboxamido-methoxytryptamine > 5-HT > 2-methyl-5-HT ≈ 5-benzyloxytryptamine ≈ tryptamine > 5-carboxamidotryptamine ≫ 5-HTQ. LSD, lisuride, 2-methyl-5-HT, tryptamine and 5-benzyloxytryptamine behaved as partial agonists relative to 5-HT. The rank order of potency of the tryptamine compounds correlated well with their affinities determined in binding assays. In addition, we have tested a number of antagonists in this system (rank order of potency: methiothepin, clozapine, mianserin and ritanserin). This characterization of the pharmacological properties of recombinant 5-HT 6 receptor will facilitate the identification of 5-HT 6 receptor-mediated responses in physiological systems. © 1997 Elsevier Science Ltd.
Neuropharmacology – Elsevier
Published: Apr 1, 1997
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