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  • Influence
Brine shrimp: a convenient general bioassay for active plant constituents.
TLDR
Screening results with seed extracts of 41 species of Euphorbiaceae were compared with 9KB and 9PS cytotoxicities and the method is rapid, reliable, inexpensive, and convenient as an in-house general bioassay tool.
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Psychedelics
  • D. Nichols
  • Psychology, Biology
    Pharmacological Reviews
  • 1 April 2016
TLDR
Blood oxygen level–dependent functional magnetic resonance imaging and magnetoencephalography have been employed for in vivo brain imaging in humans after administration of a psychedelic, and results indicate that intravenously administered psilocybin and LSD produce decreases in oscillatory power in areas of the brain’s default mode network.
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Functional Selectivity and Classical Concepts of Quantitative Pharmacology
TLDR
Besides the heuristically interesting nature of functional selectivity, there is a clear impact on drug discovery, because this mechanism raises the possibility of selecting or designing novel ligands that differentially activate only a subset of functions of a single receptor, thereby optimizing therapeutic action.
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Serotonin receptors.
2. Classification of Serotonin Receptors 1625 2.1. Gq/11-Coupled Receptor Types 1626 2.1.1. The 5-HT2A Receptor 1626 2.1.2. The 5-HT2B Receptor 1627 2.1.3. The 5-HT2C Receptor 1628 2.2. Gs-Coupled…
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Differences between the mechanism of action of MDMA, MBDB, and the classic hallucinogens. Identification of a new therapeutic class: entactogens.
  • D. Nichols
  • Medicine
    Journal of psychoactive drugs
  • 1 October 1986
The widc,pre.ld u e of psychedelic drug • ,>uch a Iy t:rgic acid dit:lh) IJmide (LSD), dunng Ihe 1960's and 1970' led 10 ev re reaclion by govern menIal agencies and pro criplion~ a '.lin~1 Iheir u…
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The G Protein–Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic with a Unique Spectrum of Activities In Vivo
TLDR
These findings provide the first evidence for a highly selective and G protein-biased tool compound for which many, but not all, of the negative side effects of KOR agonists can be minimized by creating G protein–biased KOR receptor agonists.
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Crystal Structure of an LSD-Bound Human Serotonin Receptor
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Stereochemical effects of 3,4-methylenedioxymethamphetamine (MDMA) and related amphetamine derivatives on inhibition of uptake of [3H]monoamines into synaptosomes from different regions of rat brain.
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Serotonin 5-Hydroxytryptamine2A Receptor-Coupled Phospholipase C and Phospholipase A2 Signaling Pathways Have Different Receptor Reserves
TLDR
The data support the hypothesis of agonist-directed trafficking in NIH3T3–5HT2A cells because structurally distinct ligands were able to induce preferential activation of the PLC or PLA2 signaling pathway and conclude that structurally different ligands can differentially regulate 5-HT 2A receptor signal transduction.
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1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
TLDR
(R)-2 is one of the most potent and selective compounds yet discovered in the in vivo drug discrimination assay, found to be a functionally selective agonist at the 5-HT(2A) receptor, having 65-fold greater potency in stimulating phosphoinositide turnover than in producing arachidonic acid release.
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