Characterization of Ultrapotent Chemogenetic Ligands for Research Applications in Nonhuman Primates.
chemogenetics
ligand-gated ion channels
pharmacokinetics
rhesus macaque
uPSEMs
varenicline
Journal
ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337
Informations de publication
Date de publication:
02 11 2022
02 11 2022
Historique:
pubmed:
25
10
2022
medline:
4
11
2022
entrez:
24
10
2022
Statut:
ppublish
Résumé
Chemogenetics is a technique for obtaining selective pharmacological control over a cell population by expressing an engineered receptor that is selectively activated by an exogenously administered ligand. A promising approach for neuronal modulation involves the use of "Pharmacologically Selective Actuator Modules" (PSAMs); these chemogenetic receptors are selectively activated by ultrapotent "Pharmacologically Selective Effector Molecules" (uPSEMs). To extend the use of PSAM/PSEMs to studies in nonhuman primates, it is necessary to thoroughly characterize the efficacy and safety of these tools. We describe the time course and brain penetrance in rhesus monkeys of two compounds with promising binding specificity and efficacy profiles in
Identifiants
pubmed: 36279419
doi: 10.1021/acschemneuro.2c00525
pmc: PMC9910343
mid: NIHMS1870419
doi:
Substances chimiques
Ligands
0
Varenicline
W6HS99O8ZO
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
3118-3125Subventions
Organisme : NIH HHS
ID : P51 OD011132
Pays : United States
Organisme : NINDS NIH HHS
ID : R21 NS106346
Pays : United States
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