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Amphetamine‐type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin
TLDR
In vitro methods determined the neurochemical mechanism of action of amphetamine, 3,4‐methylenedioxymethamphetamine (MDMA), (+)‐methamphetamine, ephedrine, phentermine, and aminorex, and demonstrated that the most potent effect of these stimulants is to release NE.
Differential effects of the novel kappa opioid receptor antagonist, JDTic, on reinstatement of cocaine-seeking induced by footshock stressors vs cocaine primes and its antidepressant-like effects in
TLDR
Depression and stress are two states during cocaine abstinence which users identify as precipitating relapse, and JDTic may have properties which attenuate both.
Structure of the human kappa opioid receptor in complex with JDTic
TLDR
Analysis of site-directed mutagenesis and ligand structure–activity relationships confirms the interactions observed in the crystal structure, thereby providing a molecular explanation for κ-OR subtype selectivity, and essential insights for the design of compounds with new pharmacological properties targeting the human λ-OR.
Buprenorphine-Induced Antinociception Is Mediated by μ-Opioid Receptors and Compromised by Concomitant Activation of Opioid Receptor-Like Receptors
TLDR
The results indicate that the antinociceptive effect of buprenorphine in mice is μ-opioid receptor-mediated yet severely compromised by concomitant activation of ORL-1 receptors.
Preferential Increases in Nucleus Accumbens Dopamine after Systemic Cocaine Administration Are Caused by Unique Characteristics of Dopamine Neurotransmission
TLDR
The lower rates for dopamine release and uptake measured in the nucleus accumbens were found to underlie the preferential increase in extracellular dopamine after cocaine, explaining the paradox that cocaine more effectively increases accumbal dopamine despite identical effects on the dopamine transporter in the two regions.
Structure of the human k-opioid receptor in complex with JDTic
TLDR
Analysis of site-directed mutagenesis and ligand structure–activity relationships confirms the interactions observed in the crystal structure, thereby providing a molecular explanation for k- OR subtype selectivity, and essential insights for the design of compounds with new pharmacological properties targeting the human k-OR.
Enantioselective Effects of Hydroxy Metabolites of Bupropion on Behavior and on Function of Monoamine Transporters and Nicotinic Receptors
TLDR
The results suggest that clinical and behavioral effects of bupropion arise from actions at nAChR as well as DA and NE transporters and that the (2S,3S)-hydroxybupropion isomer may be a better drug candidate for smoking cessation because of its higher potency at the relevant targets.
Varenicline Is a Partial Agonist at α4β2 and a Full Agonist at α7 Neuronal Nicotinic Receptors
TLDR
It is remarkable that varenicline is a potent, full agonist at α7 receptors with an EC50 of 18 ± 6 μM and an efficacy of 93 ± 7% (relative to acetylcholine).
Anxiolytic-Like Effects of κ-Opioid Receptor Antagonists in Models of Unlearned and Learned Fear in Rats
TLDR
The results indicate that KOR antagonists produce a unique combination of antidepressant- and anxiolytic-like effects and suggest that this class of drugs may be particularly effective for the treatment of comorbid depressive and anxiety disorders.
Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.
TLDR
It is remarkable that varenicline is a potent, full agonist at alpha7 receptors with an EC50 of 18 +/- 6 microM and an efficacy of 93 +/- 7% (relative to acetylcholine).
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