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Duchemin AM, Quach TT, Rose C, Schwartz JC. 
“Pharmacological Characterization of 3H-LSD Binding Sites in Mouse Brain In Viva”. 
Life Sci.. 1979;24(5):401-09.
3H-LSD binding sites in the mouse brain were pharmacologically characterized Methods Male Swiss albino 18-20 g mice were i.v. injected with 50 mcCi/kg (l mcg/kg) 3H-LSD at various times before sacrifice. Various brain areas were dissected and homogenized and the radioactivity (RA) counted. The effects of injection of 5-HT agonists and antagonists on the specific accumulation of 3H-LSD were determined. Results 2 Min after 3H-LSD injection, substantial levels of RA were detected in the brain. Maximal levels were found between 15-60 min. and the highest accumulation occurred in the cortex and lowest in the cerebellum. When cold d-LSD (Sandoz; 0.5 mg/kg) was given with 3H-LST), the RA accumulated into the cerebellum 1 hr later, was not affected but that in the cortex, hippocampus, striatum, hypothalamus, midbrain and brain stem was reduced to the cerebellar level. After 4 hr. the levels of RA were less affected by d-LSD. Half-maximal specific accumulation occurred with 30+5'mcg/kg, whereas maximal accumulation was achieved with 100 mcg/kg. Maximal capacity was 210+12 fmole/mg protein. Cyproheptadine, methiothepin and methysergide (Sandoz) inhibited 3H-LSD uptake with ID50 values of 0.1 mg/kg (i.v.l :Cinanserin and mianserin were less potent. Dimethyltryptamine (Sigma), psilocin (Sandoz) and psilocybin (Sandoz) significantly inhibited 3H-LSD uptake. The ID50 for dimethyltryptamine was 2.5 mgkg. Quipazine significantly inhibited 3H-LSD uptake; the effect was not dose-related. Combined 5-hydroxytryptophan plus pargyline inhibited uptake but tryptophan (Merck), DOPA and l-histidine (Merck) were inactive. Spiperone and haloperidol (Lebrun) inhibited uptake but 1 mg/kg pimozide (Lebrun) was inactive. The following were also inactive: i.v. tryptamine; N-methyltryptamine; N,N-dimethyltryptamine; 5-methoxydimethyltryptamine; 5methoxytryptamine; bufotenine (Sigma); scopolamine (Houde; 2.5 mg/kg); atropine (Houde; 5 mg/kg); morphine (25 mg/kg); i.p. chlorimipramine (40 mg/kg?; desipramine (40 mg/kg; both CIBA-Geigy) i.v. propranolol (1 mg/kg); salbutamol (0.3 mg/kg; Glaxo) and i.p. L-hitidine (Merck).
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