Trace Amine-associated Receptor (TAAR) Agonist

RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages.

ZH8651 is an orally active TAAR1 agonist. ZH8651 activates the Gs and Gq signaling pathways. ZH8651 alleviates dizocilpine-induced hyperactivity, improves prepulse inhibition deficits, and attenuates cognitive impairment in mice. ZH8651 can be used for the research of schizophrenia.

LK00764 is a TAAR1 agonist with an EC₅₀ of 4 nM. LK00764 alleviates Dizocilpine (HY-15084B)-induced hyperlocomotion, reduces vertical locomotor activity, attenuates spontaneous hyperlocomotion in dopamine transporter knockout rats, and inhibits stress-induced hyperthermia in rats. LK00764 can be used for the research of schizophrenia.

RO5192022 is a TAAR1 agonist and a radioligand for TAAR1 binding assays. RO5192022 exhibits antipsychotic-like properties. RO5192022 can be used in studies related to schizophrenia.

TAAR1-agonist-4 is a TAAR1 agonist and oral hypoglycemic agent with an EC₅₀ of 0.0046 μM for TAAR1. TAAR1-agonist-4 alleviates antipsychotic-related metabolic side effects, improves negative and cognitive symptoms, and reduces drug abuse behaviors. TAAR1-agonist-4 is applicable to research on schizophrenia, acute manic episodes associated with bipolar disorder, and glucose intolerance.

RO5166017 is an orally active and species-crosses TAAR1 agonist, with K_i values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.

Ractopamine hydrochloride (LY031537) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine hydrochloride also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine hydrochloride promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine hydrochloride can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC₅₀ value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.

ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC₅₀: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research.

Ractopamine-¹³C₆ is the ¹³C-labeled Ractopamine (HY-113781). Ractopamine (LY031537 free base) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

Gαq/11 protein-IN-1 (compound F33) is an inhibitor of Gαq/11 protein with an IC₅₀ value of 9.4 μM. Gαq/11 protein-IN-1 has antitumor activity.

TAAR1 agonist 1 hydrochloride (6e·HCl) is a novel G-protein-coupled receptor TAAR1 agonist. TAAR1 agonist 1 hydrochloride is used in the study of schizophrenia.

TAAR1 agonist 1 (compound 6E) is a potent TAAR1 agonist with a potent TAAR1-Gs/Gq dual-pathway activation property. TAAR1 agonist 1 significantly alleviates MK-801-induced schizophrenia-like cognitive phenotypes.

ZH8667 is a trace amine-associated receptor 1 (TAAR1) –Gs agonist. ZH8667 can be used for the research of schizophrenia.

Ractopamine-¹³C₂ is the ¹³C-labeled Ractopamine (HY-113781). Ractopamine (LY031537 free base) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

6-APDB hydrochloride is a trace amine-associated receptor 1 agonist. It is also a regulator of 5-hydroxytryptamine receptor and a inhibitor of sodium-dependent noradrenaline transporter inhibitor.

RO 5073012 is a selective, orally active and brain-penetrant TAAR1 agonist. RO 5073012 shows a K_i of 6 nM for hTAAR1 and EC₅₀ values of 23 and 25 nM for mTAAR1 and rTAAR1. RO 5073012 can be used for the research of neurological disease, such as schizophrenia.

TAAR1/5-H-2CR agonist-1 (compound 21b) is a TAAR1 and 5-HT_2CR dual agonist with EC₅₀s of 0.022 and 0.246 μM, respectively. TAAR1/5-H-2CR agonist-1 can used in the study of schizophrenia and Alzheimer's Disease.

Ractopamine (LY031537 free base) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC₅₀=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC₅₀=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases.