ACS Central Science
December 27, 2017
Jeremy J Roach, Yusuke Sasano, Cullen L. Schmid et al.
Salvinorin A (SalA) is a plant metabolite that agonizes the human kappa-opioid receptor (κ-OR) with high affinity and high selectivity over mu- and delta-opioid receptors. Its therapeutic potential has stimulated extensive semisynthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has been...
ChemRxiv
August 19, 2017
Jeremy J Roach, Yusuke Sasano, Cullen L. Schmid et al.
preprint
Salvinorin A (SalA) is a plant metabolite that agonizes the human kappa -opioid receptor (κ-OR) with high affinity and high selectivity over mu- and delta- opioid receptors. Its therapeutic potential has stimulated extensive semi-synthetic studies and total synthesis campaigns. However, structural modification of SalA has been complicated by its instability, and efficient total synthesis has...
Biological Psychiatry
April 15, 2012
Peter T Nguyen, Cullen L. Schmid, Kirsten M Raehal et al.
Cannabinoid CB(1) receptors (CB(1)Rs) mediate the effects of ▵(9)-tetrahydrocannabinol (THC), the psychoactive component in marijuana. Repeated THC administration produces tolerance and dependence, which limit therapeutic development. Moreover, THC produces motor and psychoactive side effects. β-arrestin2 mediates receptor desensitization, internalization, and signaling, but its role in these...
Journal of Neuroscience
October 6, 2010
Cullen L. Schmid, Laura M Bohn
172 citations
Hallucinogens mediate many of their psychoactive effects by activating serotonin 2A receptors (5-HT 2A R). Although serotonin is the cognate endogenous neurotransmitter and is not considered hallucinogenic, metabolites of serotonin also have high affinity at 5-HT 2A R and can induce hallucinations in humans. Here we report that serotonin differs from the psychoactive N -methyltryptamines by its...
The FASEB Journal
April 1, 2010
Cullen L. Schmid, Laura M Bohn
Serotonin and the hallucinogenic metabolites of tryptamines, dimethylated tryptamines, activate the serotonin 2A receptor (5‐HT2AR), which is implicated in numerous mental health disorders. We have previously demonstrated that the 5‐HT2AR is differentially regulated by βarrestin2 (βarr2) depending upon the agonist; here we utilized βarr2 knockout mice to compare signaling profiles in vivo, by...