gabaa receptor agent1

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

Antiulcer Agent 1 is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration.

anti-TB agent 1 is a potent and orally active anti-tuberculosis agent (MICs: < 2 nM against the Mtb strains H37Rv, rRMP and rINH).

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate is a synthetic compound belonging to the curcumin family. It is involved in the regulation of immune response and inflammation through inhibition of the NF-κB signaling pathway, in the regulation of antioxidant response through activation of the Nrf2 signaling pathway, and in the regulation of cell survival and proliferation through inhibition of the Akt signaling pathway.

Acetic acid, 2-[4-[(2-ethyl-3-benzofuranyl)carbonyl]phenoxy]- is a compound used for antiviral activity determinations.

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

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

Anticonvulsant agent 1 is an anticonvulsant compound.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [1].

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1, exhibiting an EC50 of 300 nM [1].

Insecticidal agent 1 exhibits greater insecticidal potency than both obacunone and toosendanin.

Succinate/succinate receptor antagonist 1 is a potent succinate receptor antagonist. Succinate/succinate receptor antagonist 1 interrupts succinate signals in gingival tissue and inhibits the activation of SucnRl Antagonist 1. Its IC50 value is 20 μsouth of the coast. Succinate/succinate receptor antagonist 1 can be used to treat periodontal disease.

Antimalarial agent 1 is an effective antimalarial agent.

Compound 3, a molluscicidal agent, is a saponin extractable from S. vesicaria [1].

Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist , has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

anti-TNBC agent-1 is a highly effective compound specifically designed to target and combat triple-negative breast cancer (TNBC). It demonstrates remarkable potency against various breast cancer cell types, with IC50 values spanning from 0.20 μM to 0.27 μM. The mechanism of action of anti-TNBC agent-1 involves inducing apoptosis in SUM-159 cells through the mitochondria pathway, as well as causing G1 phase arrest in these cells.

Glucocorticoid Receptor Agonist-1 Phosphate Gly-Glu (TFA) serves as a cleavable linker for the synthesis of Antibody-Drug Conjugates (ADCs).

Therapeutic Agent-1, a heteroaryl compound, serves as an enzyme replacement therapy to enhance glucocerebrosidase activity in the treatment of Gaucher disease [1].

Compound 11, labeled as a weak Hepatoprotective agent-1, is a naturally occurring substance extracted from the fruits of Arctium lappa L. It demonstrates modest hepatoprotective effects when applied at a concentration of 10 μM [1].

Herbicidal agent 1 ((S)-6q) exhibits superior activity compared to its racemic form [1].

Anti-MI/R injury agent 1 (compound 18), derived from Panaxatriol, represents an orally administered, potent agent against myocardial ischemia/reperfusion (MI/R) injury. It improves cell viability in cardiomyocytes subjected to oxygen-glucose deprivation and reperfusion (OGD/R)-induced injury. Furthermore, this compound significantly reduces myocardial infarction size, diminishes levels of circulating cardiac troponin I (cTnI), and mitigates cardiac tissue damage in rat models [1].

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor. It demonstrates a significant affinity for the β2 adrenoceptor, indicated by an EC50 value of 9.2 nM, and for the muscarinic receptor with a Ki value of 30.2 nM. Furthermore, its MABA activity is highlighted by an EC50 value of 4.0 nM [1].

σ1 Receptor antagonist-1 is a selective sigma 1 receptor antagonist.

GABAA receptor agent 1 has strong anticonvulsant activity and is a high affinity ligand of GABAA receptor.

Anti-amyloid agent-1 is a potent compound that inhibits amyloid aggregation, offering a promising approach for research into the treatment of amyloidosis [1].

Compound 3l, a paclitaxel derivative known as Microtubule Stabilizing Agent-1, effectively enhances tubulin polymerization and demonstrates antitumor efficacy [1].

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

Anti-Trypanosoma cruzi agent-1 (Compd E5) has a potent anti-Toxoplasma effect.

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

Anti-neurodegeneration agent 1 a neurodegeneration-targeting agent.

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].