neuropsychiatric

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.

Brilaroxazine (RP5063) is a potent multimodal dopamine 5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

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.

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

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.

Lu AF90103 (Compound 42e) is the methyl ester prodrug of compound 42d, capable of crossing the blood-brain barrier. Compound 42d acts as a partial agonist of the GluN1 GluN2B complex, with an efficacy of 24% and an EC50 value of 78 nM. Lu AF90103 plays a significant role in neuropsychiatric disorder research.

Mecamylamine hydrochloride (Mevasin) is a nicotinic antagonist, used as a ganglionic blocker in hypertension.

RO5203648 HCl is a partial agonist of trace amine-related receptor 1 (TAAR1) with antipsychotic and antidepressant-like activities. RO5203648 HCl can be used in studies about neuropsychiatric therapeutics.

SAR502250 is a potent, selective, ATP-competitive, orally active, and brain-penetrant GSK3 inhibitor with a human GSK-3β IC50 value of 12 nM, exhibiting antidepressant-like activity and being researched for potential application in Alzheimer's disease (AD) treatment.

CMPI hydrochloride, a potent and selective nAChR agonist, functions as a positive allosteric modulator (PAM) specifically targeting the α4:α4 subunit interface of the nAChR. It enhances the response of the (α4)3(β2)2 nAChR to acetylcholine (ACh) (10 μM) with an EC 50 of 0.26 μM. With its potential for researching nicotine dependence and various neuropsychiatric conditions linked to reduced brain cholinergic activity, CMPI hydrochloride stands as a significant compound in neurological research.

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.

Pifoxime, a non-steroidal anti-inflammatory agent (NSAID) and COX-1 2 inhibitor, exhibits anti-inflammatory properties, making it useful in neuropsychiatric research.

GPR52 receptor modulator 1, a compound delineated as per Procedure 1, is a modulator of the GPR52 receptor, offering research potential in the investigation of neuropsychiatric diseases [1].

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.

Cerpegin, a pyridine ketone fused c-lactone, acts as an inhibitor of the 20S proteasome. It possesses pharmacological properties as a neuropsychiatric sedative, anti-inflammatory, analgesic, and exhibits anti-ulcer activity.