at-2 receptor

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

Buloxibutid (AT2 receptor agonist C21) is a novel and selective small molecule angiotensin II AT2 receptor agonist, exhibiting Ki values of 0.4 nM and 10 μM for AT2 and AT1 receptors, respectively.

BIBS 39 is a novel nonpeptide angiotensin II (AII) receptor antagonist.

PD 123319 ((S)-(+)-PD 123319) is a potent, selective AT2 angiotensin II receptor antagonist.

Tasosartan (WAY-ANA 756) is an antagonist of angiotensin II type 2 (AT2) receptor (IC50 = 1.2 nM).

PD 123319 ditrifluoroacetate is a selective, non-peptide angiotensin II type 2 (AT2) receptor antagonist, and PD 123319 ditrifluoroacetate demonstrates potent activity with IC50 values of 34 nM in rat adrenal tissue and 210 nM in rat brain, thereby providing a valuable pharmacological tool for elucidating AT2 receptor function in cardiovascular and renal physiology and supporting research in hypertension and related disorders.

AT2 receptorligand-1 (compound 14) is a potent ligand for the angiotensin AT2 receptor, with a Ki value of 4.9 nM. It exhibits high stability in microsomes containing sulfonamide ligands.

CL-329167 (compound 12) is an orally active, competitive angiotensin II receptor antagonist (IC50=6 nM) suitable for hypertension research.

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg/kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg/kg and prevents memory deficits induced by the AMPA/kainate glutamate receptor antagonist NBQX at 0.1 mg/kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

3-(2-aminopropyl)phenol hydrochloride is a phenethylamine analog used as a molecular structural unit. It is a psychoactive drug that is a partial agonist at several serotonin receptors, including 5-HT1A, 5-HT1B, and 5-HT2C, as well as an antagonist at the 5-HT2A receptor.

2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine is an indoleamine compound that is structurally similar to serotonin. It is a selective agonist at the 5-HT2A receptor and has potential applications in neuroscience.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action related to wakefulness and cognition, and it has potential as a treatment for ADHD. In a clinical trial, the mean change from baseline in the total ADHD-RS-IV score at day 42 was -8.8 in the placebo group versus -9.3, -11.2, and -12.2 in the bavisant 1 mg/day, 3 mg/day, and 10 mg/day groups, respectively; however, the change in the 10 mg/day group was not statistically superior to placebo (p=0.161). Statistical comparisons of the 1 mg/day and 3 mg/day groups with placebo based on a step-down closed testing procedure were not performed. Bavisant has completed a phase II ADHD trial, but no results have been reported [1]. Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2. IC50 Value: Target: H3 receptor in vitro.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, shows promise as a therapeutic candidate for xerostomia in Sjogren's syndrome. It exhibits a broad pharmacological profile across various systems in animal models including mice, rats, guinea pigs, rabbits, and dogs. Metabolism studies using rat and dog liver microsomes reveal rapid absorption with peak plasma concentrations (Cmax) within one hour post-oral administration and a half-life (t1/2) between 0.4 to 1.1 hours. Bioavailability is 50% in rats and 30% in dogs. Metabolic analysis shows species-specific differences: rats produce S- and N-oxidized metabolites, while dogs produce only N-oxidized metabolites. Sex-based pharmacokinetic differences were noted in rats but not in dogs. In vitro studies indicate cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) involvement in the sulfoxidation and N-oxidation of SNI-2011, with CYP2D and CYP3A mainly responsible for sulfoxidation in rat liver microsomes.

7α,25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist, as well as an endogenous ligand, of the orphan GPCR receptor EBI2 (GPR183). It serves as a chemokine directing the migration of B cells, T cells, and dendritic cells and exhibits high potency in activating EBI2 (EC50=140 pM; Kd=450 pM) [1][2].

Bifenazate is a positive allosteric modulator of GABA receptor. Bifenazate is an acaricide that controls 100% of mites at a concentration of 25 ppm.

TC13172 is a potent and covalent inhibitor that specifically targets the mixed lineage kinase domain-like protein (MLKL), exhibiting significant selectivity for MLKL over the closely related receptor-interacting serine/threonine kinase 1 (RIPK1) and RIPK3 at a concentration of 10 µM.TC13172 effectively inhibits necroptosis induced by the TSZ combination (TNF-α, a Smac mimetic, and Z-VAD-FMK) in HT-29 cells with a EC50 of 2 nM and, at 100 nM, blocks TSZ-induced oligomerization and plasma membrane translocation of MLKL.

VU0467485 is a potent and selective muscarinic acetylcholine receptor 4 positive allosteric modulator. VU0467485 potentiates the activity of ACh at M4 (EC50s: 26.6 nM and 78.8 nM at the rat and human M4 receptors, respectively). VU0467485 displays selecti

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

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.

KR-31080, an imidazo[4,5-b]pyridine derivative, functions as an inhibitor of the angiotensin II receptor. At a concentration of 2 μm, KR-31080 reduces the production of NO in LPS-stimulated BV-2 cells by 8.3%.

25CN-NBMD is a highly selective serotonin 5-HT2A receptor (5-HT2AR) agonist developed to investigate the expression and function of 5-HT2AR. Structural modifications were made at the 2' and 3' positions of 25CN-NBMD, and studies revealed these changes are crucial for 5-HT2AR activity. This compound effectively induces characteristic responses associated with 5-HT2AR activation.