receptor modulator

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

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.

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

GLP-1 Receptormodulator 1 (Compound 7) is an effective positive allosteric modulator of the GLP-1 receptor. It is utilized in the research of obesity and type 2 diabetes.

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.

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor, demonstrating negative modulation by inhibiting receptor activity and exhibiting high selectivity towards the GluN2B subunit, with an IC50 value of 31 nM.

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].

NMDA receptor modulator 5 (Compound 195), a potent NMDA receptor modulator, shows promise for neurological disorder research [1].

σ 1 Receptor μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

NMDA receptor regulator 6 (Compound 183) is an effective NMDA receptor regulator and has research value in neurological disorders.

GABAA receptor modulator-2 (Compound 20) is a selective, orally active α5-GABAAR negative conformation modulator (Ki: 4.1 nM) that exhibits high metabolic stability and a good central nervous system safety profile.

Glucocorticoid receptor modulator 1 is a highly effective and orally administered NF-κB and AP-1 inhibitor with IC50 values of 9 nM and 130 nM, respectively. It can downregulate the expression of inflammatory factors IL-6, IL-1β, TNF-α, and MMP-13, thereby alleviating skin inflammation.