cholinergic receptor, nicotinic, α 5

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

GABAA Receptor Agent 5 (compound 018) serves as a potent γ-GABAAR antagonist, possessing a Ki of 0.020 μM. This compound exhibits γ-GABAAR antagonist properties, yet it demonstrates low cellular membrane permeability [1].

5-HT6 5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

RXFP1 receptor agonist-5 (Example 98) is an agonist targeting the RXFP1 receptor, inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, with an EC50 of 1.3 nM [1].

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

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor, specifically stimulating the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors with EC50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].

Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).

NMDA receptor antagonist 5 (Compound 10e), a potent and non-toxic agent with brain permeability, is significant for studying neurological disorders [1].

AMPA Receptor Modulator-5 (Example 217) serves as an AMPA receptor modulator, utilized in neurological disease research [1].

Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties. It additionally suppresses the synthesis of IL-17A, IL-17F, and INF-γ.

APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50: 0.4 nM) with excellent pharmacokinetic profiles in rodent heart failure (HF) models and an acceptable safety profile in preclinical toxicology studies, improving cardiac function and useful for HF disease research.

Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect in LNCaP xenograft mice model, which can be used to study prostate cancer.

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier, with an EC50 of 1.14 nM and a Ki of 0.37 nM. Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Estrogen receptor antagonist 5 is a potent inhibitor of the Estrogen receptor, a ligand-activated transcriptional regulatory protein that interacts with endogenous estrogens and mediates various biological effects. [Estrogen receptor antagonist 5] shows promise for studies on metastatic disease.

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].

Compound 42, a 5-HT6/5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT7 receptor ligand 1 (Compound 5c) is a potent 5-HT7 receptor ligand with a K i value of 8 nM, exhibiting non-hepatotoxic properties and moderate potential for drug-drug interactions with CYP3A4 or CYP2D6 substrates [1].

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

Thrombin Receptor Activator for Peptide is also called Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), used in the research of coronary heart disease (CHD).