Drug Discrimination Assay Research Articles

Studies of the relationship between molecular structure and hallucinogenic activity

The nature of the stereochemistry and aromatic ring substituents and their importance to biological activity for phenethylamine-type hallucinogens is presented. The possibility of a hydrophobic site to bind to the 4-substituent and its likely geometry is described. A brief discussion of the structure-activity relationships for tryptamines such as psilocin and DMT is also given, with comments abouth th stereochemistry of alpha-methyltryptamines. Evaluation of a series of N(6)-alkyl-nor-LSD derivatives indicated that selected members such as N(6)-ethyl, allyl and propyl were as potent as, if not more potent than LSD, both in a two-lever drug discrimination assay in rats, and in man. N(6)-alkyl groups longer than n-propyl, such as n-butyl or 2-phenethyl, gave compounds that were greatly reduced in activity.

ChemInform Abstract: SYNTHESIS AND LSD‐LIKE DISCRIMINATIVE STIMULUS PROPERTIES IN A SERIES OF N(6)‐ALKYL NORLYSERGIC ACID N,N‐DIETHYLAMIDE DERIVATIVES

AbstractGemäß Formelschema erhält man die Verbindungen (IV), die mit LSD verglichen werden.

Characterization of the interaction of pentazocine and tripelennamine: Drug discrimination and mu-receptor binding assay

Abuse of the combination of pentazocine (P) and tripelennamine (T) reputedly produces an opiate-like euphoria not obtainable from either drug alone. To determine if this effect is related to interactions at the behavioral or receptor levels we tested this combination in rats trained to discriminate morphine from saline and in mu-receptor binding assays. Displacement of 3H-DHM was compared in morphine-naive, dependent and withdrawn states to determine the importance of prior morphine exposure. The morphine training cue (3 mg/kg) generalized to P but not to T. Combinations of T (0.3 and 1.0 mg/kg) with "no effect" doses of P (1 and 3 mg/kg) resulted in greater than additive increases in morphine-like responding. 3H-DHM was displaced by P but not T in naive, dependent and withdrawn states. Specific dose combinations of T (1 nM) with P (1 nM, 10 nM, 100 nM) resulted in enhanced displacement of 3H-DHM and was not related to prior morphine exposure. We conclude that the addition of T to P increases the mu-like subjective effects of P and this effect may be due to enhanced affinity of P for the mu-receptor.