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α4β2 Nicotinic Receptors with High and Low Acetylcholine Sensitivity: Pharmacology, Stoichiometry, and Sensitivity to Long-Term Exposure to Nicotine
The effects of long-term exposure to nicotine on HS and LS receptors expressed in Xenopus laevis oocytes after cDNA injections or microtransplantation of α4β2 receptors assembled in human embryonic kidney 293 cells are evaluated.
Functional Selectivity of Hallucinogenic Phenethylamine and Phenylisopropylamine Derivatives at Human 5-Hydroxytryptamine (5-HT)2A and 5-HT2C Receptors
The results support the concept of functional selectivity and indicate that subtle changes in ligand structure can result in significant differences in the cellular signaling profile.
Glutathione transferase M2-2 catalyzes conjugation of dopamine and dopa o-quinones.
Human glutathione transferase M2-2 prevents the formation of neurotoxic aminochrome and dopachrome by catalyzing the conjugation of dopamine and dopa o-quinone with glutATHione, and both conjugates were found to be resistant to oxidation by biological oxidizing agents.
Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5‐HT2A and 5‐HT2C receptors
The pharmacological profile of a series of (±)‐2,5‐dimethoxy‐4‐(X)‐phenylisopropylamines (X=I, Br, NO2, CH3, or H) and corresponding phenylethylamines, was determined in Xenopus laevis oocytes
6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
6-Bromoflavone, obtained by bromination of flavanone, binds to central benzodiazepine receptors with a Ki=70 nM and has a clear anxiolytic activity in mice, at 0.5 mg/kg i.p. A survey of the
Molecular Determinants for Competitive Inhibition of α4β2 Nicotinic Acetylcholine Receptors
Homology modeling predicted strong ionic interactions between the ammonium center of the Erythrina alkaloids and β2Asp196, leading to the uncapping of loop C and abolished sensitivity to inhibition by DHβE or erysodine but not by epierythratidine, which is not predicted to form ionic bonds with β2 asp196.