N1‐Methyl‐2‐125I‐Lysergic Acid Diethylamide, a Preferred Ligand for In Vitro and In Vivo Characterization of Serotonin Receptors
@article{Hoffman1987N1Methyl2125ILysergicAD, title={N1‐Methyl‐2‐125I‐Lysergic Acid Diethylamide, a Preferred Ligand for In Vitro and In Vivo Characterization of Serotonin Receptors}, author={B. Hoffman and U. Scheffel and J. R. Lever and M. Karpa and P. Hartig}, journal={Journal of Neurochemistry}, year={1987}, volume={48} }
Abstract: Methylation of 2‐125I‐lysergic acid diethylamide (125I‐LSD) at the N1 position produces a new derivative, N1‐methyl‐2‐125I‐lysergic acid diethylamide (125I‐MIL), with improved selectivity and higher affinity for serotonin 5‐HT2 receptors. In rat frontal cortex homogenates, specific binding of 125I‐MIL represents 80–90% of total binding, and the apparent dissociation constant (KD) for serotonin 5‐HT2 receptors is 0.14 nM (using 2 mg of tissue/ml). 125I‐MIL also displays a high affinity… CONTINUE READING
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