Rare cis-configured 2,4-disubstituted 1-alkylpiperidines: synthesized and tested against trace-amine-associated receptor 1 (TAAR1)
Sign Up to like & getrecommendations! Published in 2021 at "Mendeleev Communications"
DOI: 10.1016/j.mencom.2021.07.016
Abstract: Abstract Rare cis-configured 2,4-disubstituted 1-alkylpyridines were envisioned as ligands for trace amine associated receptor 1 (TAAR1). They were synthesized in diastereomerically pure form with the decarboxylative Castagnoli–Cushman reac-tion followed by two reduction events. Despite showing… read more here.
Keywords: cis configured; rare cis; trace amine; taar1 ... See more keywords
Review of the Trace Amine-Associated Receptor 1 (TAAR1) Agonist Ulotaront: Part II—Summary of Initial Clinical Efficacy/Safety Results
Sign Up to like & getrecommendations! Published in 2023 at "CNS Spectrums"
DOI: 10.1017/s1092852923001372
Abstract: Abstract Introduction Ulotaront is a trace amine-associated receptor 1 (TAAR1) agonist with serotonin 5-HT1A agonist activity that has received FDA Breakthrough Therapy Designation for the treatment of schizophrenia. Here we summarize ongoing clinical research characterizing… read more here.
Keywords: safety; efficacy; trace amine; taar1 agonist ... See more keywords
Review of the TAAR1 Agonist Ulotaront: Part I—From Discovery to Clinic
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DOI: 10.1017/s1092852923001384
Abstract: Abstract Introduction Trace amine-associated receptors (TAARs) are a family of G-protein-coupled receptors (GPCRs) first identified in 2001. TAAR1 has emerged as a promising therapeutic target due to its ability to modulate monoaminergic and glutamatergic neurotransmission.… read more here.
Keywords: pharmacology; trace amine; taar1 agonist; discovery ... See more keywords
Trace amine associated receptor 1 (TAAR1) expression and modulation of inflammatory cytokine production in mouse bone marrow-derived macrophages: a novel mechanism for inflammation in ulcerative colitis
Sign Up to like & getrecommendations! Published in 2019 at "Immunopharmacology and Immunotoxicology"
DOI: 10.1080/08923973.2019.1672178
Abstract: Abstract Context: Tissue resident macrophages and peripherally infiltrating macrophages play a prominent role in maintaining homeostasis in the gastrointestinal tract (GIT), though aberrant activation is implicated in inflammatory conditions, including ulcerative colitis (UC). Recent metabolomic… read more here.
Keywords: inflammatory cytokine; taar1 expression; ulcerative colitis; expression ... See more keywords
Evolution of Brain-Expressed Biogenic Amine Receptors into Olfactory Trace Amine-Associated Receptors
Sign Up to like & getrecommendations! Published in 2022 at "Molecular Biology and Evolution"
DOI: 10.1093/molbev/msac006
Abstract: Abstract The family of trace amine-associated receptors (TAARs) is distantly related to G protein-coupled biogenic aminergic receptors. TAARs are found in the brain as well as in the olfactory epithelium where they detect biogenic amines.… read more here.
Keywords: associated receptors; brain; trace amine; amine associated ... See more keywords
A partial trace amine‐associated receptor 1 agonist exhibits properties consistent with a methamphetamine substitution treatment
Sign Up to like & getrecommendations! Published in 2017 at "Addiction Biology"
DOI: 10.1111/adb.12410
Abstract: Recent evidence suggests that the trace amine‐associated receptor 1 (TAAR1) plays a pivotal role in the regulation of dopamine (DA) transmission and psychostimulant action. Several selective TAAR1 agonists have previously shown efficacy in models of… read more here.
Keywords: taar1; trace amine; associated receptor; amine associated ... See more keywords
Validation of a High-Throughput Calcium Mobilization Assay for the Human Trace Amine-Associated Receptor 1
Sign Up to like & getrecommendations! Published in 2020 at "SLAS Discovery"
DOI: 10.1177/2472555220945279
Abstract: The human trace amine-associated receptor 1 (hTAAR1) is a G protein-coupled receptor (GPCR) that is widely expressed in monoaminergic nuclei in the central nervous system and has therapeutic potential for multiple diseases, including drug addiction… read more here.
Keywords: htaar1; human trace; calcium; mobilization ... See more keywords
Trace Amine-Associated Receptors as Novel Therapeutic Targets for Immunomodulatory Disorders
Sign Up to like & getrecommendations! Published in 2018 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2018.00680
Abstract: Trace amines and their receptors (trace amine-associated receptors; TAARs) are an emerging pharmacological target for the treatment of human disorders. While most studies have focused on their therapeutic potential for neurologic and psychiatric disorders, TAARs… read more here.
Keywords: immunomodulatory disorders; associated receptors; trace amine; amine ... See more keywords
Deregulation of Trace Amine-Associated Receptors (TAAR) Expression and Signaling Mode in Melanoma
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DOI: 10.3390/biom12010114
Abstract: Trace amine-associated receptors (TAARs) interact with amine compounds called “trace amines” which are present in tissues at low concentrations. Recently, TAARs expression in neoplastic tumors was reported. In this study, TAARs expression was analyzed in… read more here.
Keywords: melanoma; associated receptors; expression; trace amine ... See more keywords
Trace Amine Associate Receptor 1 (TAAR1) as a New Target for the Treatment of Cognitive Dysfunction in Alzheimer’s Disease
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23147811
Abstract: Worldwide, approximately 27 million people are affected by Alzheimer’s disease (AD). AD pathophysiology is believed to be caused by the deposition of the β-amyloid peptide (Aβ). Aβ can reduce long-term potentiation (LTP), a form of… read more here.
Keywords: cognitive dysfunction; taar1; alzheimer disease; trace amine ... See more keywords