neuropsychiatric

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

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.

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.

ARN25657 is a dual regulator of D3R/GSK-3β. It demonstrates partial agonist activity at the D3 receptor (EC50 = 15.2 nM, Ki = 1.5 nM) alongside potent inhibitor activity against GSK-3β (IC50 = 19.3 nM). ARN25657 shows excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. It inhibits P-gp-mediated efflux of acetoxymethyl calcein, enhancing in vitro ADME properties while maintaining balanced dual-target distribution. ARN25657 is applicable in the study of bipolar disorder and related neuropsychiatric conditions.

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.

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.