Abcam, ab254331, EPPTB, TAAR1 antagonist

Size: 10mg / 50mg
MW 378.4 Da, Purity >99%. Novel, selective, highly potent trace amine associated receptor 1 (TAAR1) antagonist. Higher potency in mouse than rat and human (IC 50 values are 28nM, 4539nM and 7487nM, respectively). Increases firing frequency of dopamine (DA)neurons in ventral tegmental area by blocking inward potassium current mediated by TAAR1, increasing DA activity on D 2 receptor. Displays inverse agonism in vitro by reducing cAMP levels (IC 50 =19nM).
Key facts
CAS number:1110781-88-8,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:378.4 Da,
Molecular formula:C20H21F3N2O2,
PubChem:25175634,
Nature:Synthetic,
Solubility:Soluble in DMSO to 50mM,
Biochemical name:Epptb,
Biological description:Novel, selective, highly potent trace amine associated receptor 1 (TAAR1) antagonist. Higher potency in mouse than rat and human (IC50 values are 28nM, 4539nM and 7487nM, respectively). Increases firing frequency of dopamine (DA)neurons in ventral tegmental area by blocking inward potassium current mediated by TAAR1, increasing DA activity on D2 receptor. Displays inverse agonism in vitro by reducing cAMP levels (IC50 =19nM).,
Canonical smiles:CCOC1=CC=CC(=C1)NC(=O)C2=CC(=C(C=C2)N3CCCC3)C(F)(F)F,
InChi:InChI=1S/C20H21F3N2O2/c1-2-27-16-7-5-6-15(13-16)24-19(26)14-8-9-18(25-10-3-4-11-25)17(12-14)20(21,22)23/h5-9,12-13H,2-4,10-11H2,1H3,(H,24,26),
InChiKey:KLFVWQCQUXXLOU-UHFFFAOYSA-N,
IUPAC Name:N-(3-ethoxyphenyl)-4-pyrrolidin-1-yl-3-(trifluoromethyl)benzamide

Product details:
Solutions in DMSO may be stored at -20°C for up to 3 months.

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions--20°C

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
TAAR1 also known as Trace Amine-Associated Receptor 1 is a G-protein-coupled receptor primarily involved in the modulation of monoaminergic systems in the brain. It has an approximate molecular mass of 37 kDa. This receptor is expressed largely in the central nervous system particularly in regions such as the prefrontal cortex amygdala and hippocampus but also found in some peripheral tissues like the pancreas. TAAR1 is responsive to trace amines which are endogenous compounds structurally related to monoamine neurotransmitters.
Biological function summary
TAAR1 influences monoaminergic activity. It plays a critical role in regulating the release and reuptake of neurotransmitters like dopamine and serotonin. It does not form part of a larger receptor complex but instead exerts its influence by interacting with proteins associated with neurotransmitter release management. TAAR1's activation produces various responses depending on the cell type and neurological context impacting mood and cognition processes.
Pathways
TAAR1 signaling integrates into dopaminergic and serotonergic pathways. It modulates the activity of these pathways by altering the concentration of neurotransmitters through interacting with dopaminergic D2 receptors and serotonin transporters. This receptor operates within these pathways by providing feedback control influencing neurotransmitter dynamics critically involved in mood regulation and behavior expression.
TAAR1 connects closely to schizophrenia and depression. Studies associate its functional activity with altered monoamine levels seen in these conditions. In schizophrenia TAAR1 has connections with dopamine dysregulation with proteins such as the D2 receptor heavily implicated in pathophysiology. In depression its modulation of serotonin transporter function may impact therapeutic outcomes. Understanding TAAR1's role in these disorders helps guide the development of novel targeted therapies.