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.

σ1R-IN-1 ((R,R)-1a) is an effective σ-1R inhibitor with an IC50 of 110 nM. It shows promising potential for use in research related to neuropsychiatric disorders.

CTW0419 is an effective positive allosteric modulator (PAM) of the 5-HT receptor, showing promise in research related to neuropsychiatric disorders.

CTW0404 is an effective positive allosteric modulator (PAM) of the 5-HT receptor, with promising implications for research into neuropsychiatric disorders.

5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1A receptor agonist with an EC50 of 0.18 nM. This compound mimics serotonin binding to receptors, promoting postsynaptic membrane depolarization, inhibiting excessive neuronal excitability, and reducing the release of neurotransmitters associated with anxiety. 5-HT1A agonist 1 holds potential for research in neuropsychiatric disorders.

GABAB receptor antagonist 5 (Compound 23) is a competitive antagonist of the GABAB receptor. It holds potential for research into neuropsychiatric disorders, including epilepsy, depression, and addiction.

5-HT1AR agonist 3 (Compound 77) is a 5-HT1A receptor agonist that exhibits receptor activation activity with an EC50 of 1.3 nM. It primarily functions by activating the 5-HT1A receptor and can be utilized in research related to neuropsychiatric conditions, such as anxiety, depression, and sleep disorders.

NOP antagonist 1 (Compound (-)-31) is an antagonist of the nociceptin/orphanin FQ peptide receptor (NOP) with a Kb value of 8.65 nM. It is applicable in research related to neuropsychiatric disorders.

CX1739 is a weak modulator of the AMPA-glutamate receptor (AMPAR). In mouse models, CX1739 enhances long-term potentiation in a dose-dependent manner. It also counteracts amphetamine-induced locomotor activity and rapidly reverses opioid-induced respiratory depression. CX1739 is applicable for research into dementia, neuropsychiatric disorders, and severe complications arising from opioid-induced suppression of endogenous inspiratory respiratory rhythms.

RS130-180 is a β-arrestin-biased agonist that selectively targets the 5-hydroxytryptamine 2A receptor (5-HT2aR). It shows promise for research in neuropsychiatric disorders such as depression.

VU6002703 (Compound 17) is a brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (mAChR), exhibiting an EC50 of 0.6 μM for hM4. This compound is useful for researching neuropsychiatric disorders and rare genetic central nervous system conditions.

Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist (PAM-antagonist) of the D3 dopamine receptor (D3R) that can cross the blood-brain barrier. It demonstrates antagonistic activity in D3R-mediated β-arrestin recruitment assays with an IC50 of 2.5 μM and Kb of 0.49 μM, and in D3R-mediated Go-BRET assays with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 is applicable for the study of neuropsychiatric disorders, including substance use disorders.

SST1 receptor antagonist-1 (Compound 23) is a selective antagonist of the somatostatin receptor 1 (SST1), showing a pKd of 9.11 for rSST1 and 8.79 for hSST1. This compound is applicable in research related to retinal and endocrine dysfunction, cancer, and 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.