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Page 1
Inside-out neuropharmacology of nicotinic drugs.
Henderson BJ, Lester HA. Henderson BJ, et al. Among authors: lester ha. Neuropharmacology. 2015 Sep;96(Pt B):178-93. doi: 10.1016/j.neuropharm.2015.01.022. Epub 2015 Feb 4. Neuropharmacology. 2015. PMID: 25660637 Free PMC article. Review.
Because these processes depend on pharmacological chaperoning within intracellular organelles, we group them as "inside-out pharmacology". This term contrasts with the better-known, acute, "outside-in" effects of activating and desensitizing plasma membrane AChRs. W …
Because these processes depend on pharmacological chaperoning within intracellular organelles, we group them as "inside-out ph …
Antidepressants enter cells, organelles, and membranes.
Blumenfeld Z, Bera K, Castrén E, Lester HA. Blumenfeld Z, et al. Among authors: lester ha. Neuropsychopharmacology. 2024 Jan;49(1):246-261. doi: 10.1038/s41386-023-01725-x. Epub 2023 Oct 2. Neuropsychopharmacology. 2024. PMID: 37783840 Free PMC article. Review.
In the current literature, mechanisms involving intracellular targets are termed "location-biased actions" or "inside-out pharmacology". Hopefully, these general terms will eventually acquire additional mechanistic details....
In the current literature, mechanisms involving intracellular targets are termed "location-biased actions" or "inside-out phar …
Selective Serotonin Reuptake Inhibitors within Cells: Temporal Resolution in Cytoplasm, Endoplasmic Reticulum, and Membrane.
Nichols AL, Blumenfeld Z, Luebbert L, Knox HJ, Muthusamy AK, Marvin JS, Kim CH, Grant SN, Walton DP, Cohen BN, Hammar R, Looger L, Artursson P, Dougherty DA, Lester HA. Nichols AL, et al. Among authors: lester ha. J Neurosci. 2023 Mar 29;43(13):2222-2241. doi: 10.1523/JNEUROSCI.1519-22.2022. Epub 2023 Mar 3. J Neurosci. 2023. PMID: 36868853 Free PMC article.
Fluorescence activation mechanism and imaging of drug permeation with new sensors for smoking-cessation ligands.
Nichols AL, Blumenfeld Z, Fan C, Luebbert L, Blom AEM, Cohen BN, Marvin JS, Borden PM, Kim CH, Muthusamy AK, Shivange AV, Knox HJ, Campello HR, Wang JH, Dougherty DA, Looger LL, Gallagher T, Rees DC, Lester HA. Nichols AL, et al. Among authors: lester ha. Elife. 2022 Jan 4;11:e74648. doi: 10.7554/eLife.74648. Elife. 2022. PMID: 34982029 Free PMC article.
Biosensors Show the Pharmacokinetics of S-Ketamine in the Endoplasmic Reticulum.
Bera K, Kamajaya A, Shivange AV, Muthusamy AK, Nichols AL, Borden PM, Grant S, Jeon J, Lin E, Bishara I, Chin TM, Cohen BN, Kim CH, Unger EK, Tian L, Marvin JS, Looger LL, Lester HA. Bera K, et al. Among authors: lester ha. Front Cell Neurosci. 2019 Nov 12;13:499. doi: 10.3389/fncel.2019.00499. eCollection 2019. Front Cell Neurosci. 2019. PMID: 31798415 Free PMC article.
Determining the pharmacokinetics of nicotinic drugs in the endoplasmic reticulum using biosensors.
Shivange AV, Borden PM, Muthusamy AK, Nichols AL, Bera K, Bao H, Bishara I, Jeon J, Mulcahy MJ, Cohen B, O'Riordan SL, Kim C, Dougherty DA, Chapman ER, Marvin JS, Looger LL, Lester HA. Shivange AV, et al. Among authors: lester ha. J Gen Physiol. 2019 Jun 3;151(6):738-757. doi: 10.1085/jgp.201812201. Epub 2019 Feb 4. J Gen Physiol. 2019. PMID: 30718376 Free PMC article.
We use these data to run combined pharmacokinetic and pharmacodynamic simulations of human smoking. In the ER, the inside-out pathway begins when nicotine becomes a stabilizing pharmacological chaperone for some nAChR subtypes, even at concentrations as low as 10 nM …
We use these data to run combined pharmacokinetic and pharmacodynamic simulations of human smoking. In the ER, the inside-out
Smoking-Relevant Nicotine Concentration Attenuates the Unfolded Protein Response in Dopaminergic Neurons.
Srinivasan R, Henley BM, Henderson BJ, Indersmitten T, Cohen BN, Kim CH, McKinney S, Deshpande P, Xiao C, Lester HA. Srinivasan R, et al. Among authors: lester ha. J Neurosci. 2016 Jan 6;36(1):65-79. doi: 10.1523/JNEUROSCI.2126-15.2016. J Neurosci. 2016. PMID: 26740650 Free PMC article.
We show that nicotine, operating via nicotinic receptors, does protect these neurons against endoplasmic reticulum stress. However, the mechanism is probably "inside-out": pharmacological chaperoning in the endoplasmic reticulum. This cellular-level insight could he …
We show that nicotine, operating via nicotinic receptors, does protect these neurons against endoplasmic reticulum stress. However, the mech …
A C-terminal peptide of the GIRK1 subunit directly blocks the G protein-activated K+ channel (GIRK) expressed in Xenopus oocytes.
Luchian T, Dascal N, Dessauer C, Platzer D, Davidson N, Lester HA, Schreibmayer W. Luchian T, et al. Among authors: lester ha. J Physiol. 1997 Nov 15;505 ( Pt 1)(Pt 1):13-22. doi: 10.1111/j.1469-7793.1997.013bc.x. J Physiol. 1997. PMID: 9409468 Free PMC article.
In order to find out the functional roles of cytosolic regions of a G protein-activated, inwardly rectifying potassium channel subunit we studied block of GIRK channels, expressed in Xenopus laevis oocytes, by synthetic peptides in isolated inside-out membrane patch …
In order to find out the functional roles of cytosolic regions of a G protein-activated, inwardly rectifying potassium channel subunit we st …
Functional expression of the heteromeric "olfactory" cyclic nucleotide-gated channel in the hippocampus: a potential effector of synaptic plasticity in brain neurons.
Bradley J, Zhang Y, Bakin R, Lester HA, Ronnett GV, Zinn K. Bradley J, et al. Among authors: lester ha. J Neurosci. 1997 Mar 15;17(6):1993-2005. doi: 10.1523/JNEUROSCI.17-06-01993.1997. J Neurosci. 1997. PMID: 9045728 Free PMC article.
We recorded conductances with the electrophysiological characteristics of the heteromeric olfactory cng channel in excised inside-out patches from these cultured neurons. We also show that Ca2+ influx into hippocampal neurons in response to cyclic nucleotide elevati …
We recorded conductances with the electrophysiological characteristics of the heteromeric olfactory cng channel in excised inside- …