receptor modulator

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

Opioid receptor modulator 1 is a modulator of the opioid receptor.

Toll-like receptor modulator is a TLR7/8 modulator that regulates immune function.

Androgen receptormodulator 3 is a selective modulator of the androgen receptor, applied in the study of muscle atrophy.

GABAA receptor modulator-3 (compound 3b) is a positive allosteric modulator (PAM). It inhibits the peak current and steady-state current of α1β3γ2 GABAAR with IC50 values of 671 μM and 64 μM, respectively.

GABAA receptor modulator-4 (Compound 4) acts as a negative allosteric modulator of the GABAA receptor. It inhibits the peak and steady-state currents mediated by the α1β3γ2 GABAA receptors, with an IC50 of 10 μM for both.

α5-GABAA receptor modulator 1 (Compound A-4) is a selective silent allosteric modulator (SAM) targeting the α5 subunit of GABAA receptors, useful for research into central nervous system (CNS) disorders.

D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.

GABAA receptor modulator-7 (compound 1m), a spirobarbiturate, acts as a modulator of the GABAA receptor. It can reverse the effects of anesthetics without interfering with GABA-induced desensitization and is applicable in the research of antiepileptic and anxiolytic drugs.

GABAA receptor modulator-8 (10c) is a selective positive modulator of the GABAA receptor that can cross the blood-brain barrier and exhibits anticonvulsant activity.

AMPA receptormodulator-7 is a modulator of the AMPA receptor. This compound is orally active and capable of crossing the blood-brain barrier.

AMPA receptormodulator-8 (Example 270) is an AMPA receptor modulator with an IC50 of 0.02 nM for TARP-γ2. It is useful in research related to neurological disorders such as epilepsy, Alzheimer's disease, and Parkinson's disease.

GABAA receptor modulator-9 is a positive allosteric modulator of the GABAA receptor, specifically targeting the α1β2γ2 subtype and capable of crossing the blood-brain barrier. It exhibits excellent activity at α1β2γ2 (EC50: 0.9 μM in oocytes and 0.2 μM in CHO cells) and also shows activity at α1β2, α3β2γ2, and α1β3γ2 (with EC50 values of 1.3, 3.4, and 1.1 μM, respectively). GABAA receptor modulator-9 significantly inhibits seizure progression and reduces mortality in mice. It is applicable in studies of status epilepticus (SE).

c-KitReceptor modulator-1 (Compound #22) is a regulator of the c-Kit receptor. This compound is applicable in research focused on malignant cancers such as canine mast cell tumors, human gastrointestinal stromal tumors, and small cell lung cancer.

NMDA receptor modulator9 is an orally active positive allosteric modulator (PAM) of the NMDA receptor. It enhances the activity of the GluN2A receptors. In a chronic restraint stress (CRS) induced depression mouse model, NMDA receptor modulator9 exhibits significant antidepressant-like effects. It is used for research on depression.

GABAA receptor modulator-10 is an orally active and potent positive allosteric modulator (PAM) of the α1β2γ2GABAA receptor, exhibiting good blood-brain barrier permeability. It enhances the function of the α1β2γ2 GABAA receptor and increases GABA-induced currents. In mouse models of epilepsy induced by Pentetrazol (PTZ) and Kainic Acid (KA), GABAA receptor modulator-10 demonstrates strong antiepileptic efficacy. This compound shows potential for epilepsy research.

GABAA receptor modulator-12 (Compound 5) is a modulator of the GABAA receptor. It inhibits anesthetic-induced desensitization of the GABAAα3β3γ2 receptor, with an IC50 of 0.2 μM. This compound is useful for research in central nervous system diseases.

AMPA receptor modulator-9 is a selective, orally active positive allosteric modulator of AMPARs, capable of crossing the blood-brain barrier. It selectively enhances AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortical primary neurons. The compound upregulates BDNF protein expression in primary rat cortical neuron cultures and enhances AMPA-mediated excitatory postsynaptic responses in rats and mice. AMPA receptor modulator-9 is applicable for cognitive disorder studies.

GABAA receptor modulator-11 (Compound 4) is a modulator of the GABAA receptor. It inhibits anesthetic-induced desensitization of GABAAα1β3γ2 and α1β3 receptors with IC50 values of 5.1 μM and 3.1 μM, respectively. GABAA receptor modulator-11 is relevant for central nervous system disease research.

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β, exhibiting remarkable affinity (K i = 0.44 nM) and impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator suitable for neurological disorder research [1].

NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator useful in neurological disorder research [1].

NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator used for neurological disorder research [1].