neuropsychiatric disorders

SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

JP1302 is a selective α2C adrenoceptor antagonist with a Kb value of 16 nM and a Ki of 28 nM for human α2C receptors.JP1302 has antidepressant activity, disrupts the FACT complex and degrades histone H1.JP1302 has been used in the study of neuropsychiatric disorders, acute renal failure, and renal injury.

VU6005806 is a potent positive allosteric modulator (PAM) of muscarinic acetylcholine receptor subtype 4 (M4) (EC50s: 94 nM, 28 nM, 87 nM, and 68 nM for human, rat, dog, and cyno M4, respectively), and used in the study of neuropsychiatric disorders.

TAAR1 agonist 3 is a potent agonist of Trace Amine-Associated Receptor 1 (TAAR1) with a pEC50 value of 7.6. Additionally, it acts as a full agonist at the α2AR with a pEC50 of 6. TAAR1 agonist 3 is utilized in the research of neuropsychiatric disorders.

hBChE-IN-4 (compound 40) serves as an effective activator for hCA and an inhibitor for BChE. It demonstrates affinity for various hCA subtypes with affinity constants (KA) of 266 nM for hCA I, 76.9 nM for hCA II, 918 nM for hCA IV, 893 nM for hCA VB, and 98.0 nM for hCA VII. Inhibition concentrations (IC50) for eeAChE and eqBChE are recorded at 72.1 nM and 4.2 nM, respectively. hBChE-IN-4 is non-cytotoxic and has demonstrated potential cognitive enhancement effects. It holds potential for research in neurodegenerative and other neuropsychiatric disorders.

ACSS2-IN-2 (MTB-9655) is an inhibitor of acyl-CoA synthetase short-chain family member 2 (ACSS2). ACSS2-IN-2 can inhibit ACSS2 activity with an IC50 value of 3.8 nM. ACSS2-IN-2 can be used for the research of several diseases, such as viral infection, metabolic disorders, neuropsychiatric diseases, inflammatory autoimmune conditions and cancer.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of less than 1 nM, suitable for studying neuropsychiatric disorders.

Mecamylamine, an orally active, nonselective, noncompetitive antagonist of nAChR (nicotinic acetylcholine receptors), exhibits ganglionic blockade capabilities and can cross the blood-brain barrier. Its applications span research areas including neuropsychiatric disorders, hypertension, and antidepressant efficacy.

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

CSD-CH2(1,8)-NH2 is a selective and competitive kappa-opioid receptor (KOR) antagonist with a K i of 6.8 nM. It inhibits calcium mobilization in dorsal root ganglion (DRG) neurons and counters the antinociceptive effect of U50,488, making it useful for research into neuropsychiatric disorders [1].

PW0729 (compound 15b) serves as an agonist for the orphan receptor GPR52, facilitating its activation and signaling bias for neuropsychiatric and neurological disorders. Further optimization of its brain exposure characteristics is required for PW0729.

Prolyl Endopeptidase is highly active in the brain and other tissues, where it degrades peptides containing proline, such as Substance P, neuropeptide Y, gonadotropin-releasing hormone, thyrotropin-releasing hormone, bradykinin, and angiotensin II. This enzyme is utilized in researching neuropsychiatric disorders including stress disorders, depression, and schizophrenia.