Distribution of 1,2,3,4‐Tetrahydro‐β‐carboline and 6‐Methoxy‐1,2,3,4‐tetrahydro‐β‐carboline in Mice

Abstract
The distribution of radioactivity after i.v. injection of 14C-labeled 1,2,3,4-tetrahydro-.beta.-carboline (THBC) and 6-methoxy-1,2,3,4-tetrahydro-.beta.-carboline (6-MeO-THBC) was studied on mice by whole-body autoradiography and by liquid scintillation counting (LSC). Following i.v. injection they rapidly distributed into different organs and were excreted into urine and the gut contents. A considerable uptake of the compounds was seen in the lungs, kidney, liver, bone marrow, urinary bladder, gastrointestinal tract and in various glands, e.g., adrenal, Harderian and salivary glands. THBC moderately penetrated the blood-brain barrier and the placenta but 6-MeO-THBC seemed to penetrate poorly both. At early stages of the experiment, the values of tissue radioactivity in LSC were generally much higher in the THBC group but 24 h following injections the reverse was true with higher activities in the 6-MeO-THBC group. The initial excretion of 6-MeO-THBC seemed to be more rapid judged by the superfluous accumulation of activity in the bladder and a high accumulation of activity into the gut contents.