Structure-activity-relationships of certain hallucinogenic substances based on brain levels.
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Biomedical subjects
Publications and source records attributed to B D Evans.
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Methods for the determination of a number of O and/or N-methylated derivatives of norepinephrine were developed. The IP injection of these compounds into rats shows quick absorption and short half-lives in plasma, liver and brain. Most compounds do not cross the Blood-Brain-Barrier (BBB) due to low lipid solubility. However, lipid solubility is not a sole determinant. Compounds which have at least one of the 2 phenolic hydroxyl groups methylated and possess a tertiary amino group do cross the BBB readily.
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Using a four-step reverse phase HPLC separation and RIA, five RFamide peptides were purified from CNS extracts of the leech Hirudo medicinalis. YMRFamide, FMRFamide, YLRFamide, FLRFamide, and GGKYMRFamide were identified by a combination of antiserum specificity in RIA, Edman degradation, and mass spectrometry. At least three of these five endogenous peptides can modulate neuromuscular interactions in the leech (38). FMRFamide-like immunoreactivity was selectively released from neural processes on isolated heart tubes in the presence of calcium and depolarizing levels of potassium.