Results 151 to 160 of about 1,835 (190)

TAAR1 as an emerging target for the treatment of psychiatric disorders

Pharmacology & Therapeutics
Trace amines, a group of amines expressed at the nanomolar level in the mammalian brain, can modulate monoamine transmission. The discovery of and the functional research on the trace amine-associated receptors (TAARs), especially the most well-characterized TAAR1, have largely facilitated our understanding of the function of the trace amine system in ...
Jun-Xu Li, Jian-Feng Liu, Ruyan Wu
exaly   +3 more sources

Pharmacologic Characterization of the Cloned Human Trace Amine-Associated Receptor1 (TAAR1) and Evidence for Species Differences with the Rat TAAR1

The Journal of Pharmacology and Experimental Therapeutics, 2007
The hemagglutinin-tagged human trace amine-associated receptor1 (TAAR1) was stably coexpressed with rat Galpha(s) in the AV12-664 cell line, and receptor activation was measured as the stimulation of cAMP formation. After blockade of endogenously expressed alpha2- and beta-adrenoceptors with 2-[2-(2-methoxy-1,4-benzodioxanyl)]-imidazoline hydrochloride
David B, Wainscott, Sheila P, Little, Tinggui, Yin, Yuan, Tu, Vincent P, Rocco, John X, He, David L, Nelson   +6 more
openaire   +2 more sources

Preclinical development of [¹⁸F]TAAR1-2203 as a PET radioligand for imaging TAAR1 expression and receptor occupancy

Purpose Trace amine-associated receptor 1 (TAAR1) is an emerging therapeutic target with various implications in neuropsychiatric and metabolic disorders. However, the absence of a suitable positron emission tomography (PET) radioligand has precluded non-invasive quantification of TAAR1 expression and drug-receptor interactions in vivo.
Haider, Achi, Xiao, Zhiwei, Chen, Jiahui, Pfister, Stefanie K., Zhou, Xin, Li, Yinlong, Chaudhary, Ahmad, Zhao, Chunyu, Rong, Jian, Paehler, Axel, Mohr, Susanne, Norcross, Roger D., Honer, Michael, Mu, Linjing, Gobbi, Luca, Schibli, Roger, Hoener, Marius C., Liang, Steven H.   +17 more
openaire   +1 more source

The potential of TAAR1 agonists in bipolar disorder

European Neuropsychopharmacology, 2022
Anna Giménez-Palomo, Eduard Vieta
openaire   +2 more sources

Optimisation of imidazole compounds as selective TAAR1 agonists: Discovery of RO5073012

Bioorganic & Medicinal Chemistry Letters, 2012
A series of imidazole compounds has been identified which affords potent and selective partial and full agonists of the TAAR1 receptor. Starting from 2-benzyl-imidazoline screening hits, a series of structurally related 2-benzyl- and 4-benzyl-imidazoles was investigated first, but it proved highly challenging to obtain compounds having sufficient ...
Guido, Galley, Henri, Stalder, Annick, Goergler, Marius C, Hoener, Roger D, Norcross   +4 more
openaire   +2 more sources

BRET Approaches to Characterize Dopamine and TAAR1 Receptor Pharmacology and Signaling

2012
It is evident that G protein-coupled receptors (GPCRs) such as D2 dopamine receptor and functionally related Trace Amine Associated Receptor 1 (TAAR1) can engage both in G protein-dependent (e.g., cAMP-mediated) and -independent β-arrestin-mediated signaling modalities.
Espinoza S, Masri B, Salahpour A, Gainetdinov RR   +3 more
openaire   +4 more sources

Structural and signaling mechanisms of TAAR1 enabled preferential agonist design

Cell, 2023
Yang Lejin, Jinpeng Sun, Kong-Kai Zhu
exaly  

Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia

ACS Medicinal Chemistry Letters, 2022
Kenneth S Koblan, Lee W Herman, Liming Shao   +2 more
exaly  

The selective TAAR1 partial agonist RO5263397 promoted novelty recognition memory in mice

Psychopharmacology, 2021
Yanan Zhang, Jun-Xu Li, Robert Seaman Jr
exaly  

Role of TAAR1 in breast cancer

2023
openaire   +1 more source