behaviors

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, exhibiting an EC50 of 25 nM in vitro cAMP functional assay. It significantly reduces alcohol reinforcement and intake behaviors in rats [1].

LY2794193, a potent and selective mGlu3 (metabotropic glutamate 3) receptor agonist, Ki=0.927 nM, EC50=0.47 nM, reduces akathisia seizures and depressive-like behaviors and increases GAT1, GLAST and GLT-1 protein levels in rats.

MAO-A/SERT-IN-1 acts as an inhibitor for both MAO-A and the serotonin transporter (SERT). It decreases the SERT-mediated reuptake of 5-HT and demonstrates neuroprotective properties in cellular inhibition models. Additionally, this compound has shown to alleviate depressive behaviors in both zebrafish and mice.

Ceramide 1-phosphate, a bioactive lipid, is a critical component of sphingolipids. It plays versatile roles in various cellular behaviors, including differentiation, migration, proliferation, and apoptosis.

RA-PR058 is an orally active Ramalin derivative capable of penetrating the blood-brain barrier, with multi-target regulatory functions. By reducing BACE1 expression, decreasing excessive tau protein phosphorylation, and mitigating anxiety-like behaviors, along with displaying favorable pharmacokinetic properties, RA-PR058 shows promise as a multi-target modulator for Alzheimer's disease.

AChE-IN-83 (compound f1) is an AChE inhibitor that suppresses nematode growth and acetylcholinesterase activity in rice seeds while being safe for the seeds. It specifically targets Aphelenchoides besseyi, with an LC50 of 19.0 μg/mL over 48 hours. AChE-IN-83 impedes nematode populations and behaviors in rice seeds, damages the nematode cuticle, and induces reactive oxygen species, lipofuscin, and lipid generation within the nematodes.

CD-10 is an orally active inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) that can penetrate the blood-brain barrier. It binds to Keap1 with a KD value of 193 nM. CD-10 exerts significant antioxidant and anti-inflammatory effects by activating the Keap1-Nrf2 pathway, demonstrated by reduced levels of MDA, IL-4, and IL-10, and increased expression of HO-1 protein. In a chronic unpredictable mild stress (CUMS) mouse model, CD-10 effectively alleviates anxiety and depressive behaviors and restores serum neurotransmitter levels by promoting Nrf2 nuclear translocation. CD-10 is applicable for research in depression.

G721-0282 is an orally active inhibitor of CHI3L1 that reduces the expression of inflammatory proteins and cytokines. It suppresses the activation of the NF-κB signaling pathway, inhibits neuroinflammation, and decreases anxiety-related behaviors. Additionally, G721-0282 significantly curtails the proliferation of osteosarcoma (OS) cells by inhibiting the STAT3 signaling pathway and induces apoptosis in OS cells by upregulating pro-apoptotic protein levels while downregulating anti-apoptotic protein levels. This compound is useful in the study of neuroinflammatory diseases and cancer.

MP1202 is a dual agonist for MOR and KOR, with EC50 values of 0.32 μM for mMOR-1 and 0.13 μM for mKOR-1. It exhibits functional selectivity by reducing β-arrestin1/2 recruitment in hMOR and hKOR while significantly activating G protein and Gα subtypes. In opioid receptor subtype knockout mouse models, MP1202 demonstrates potent antinociceptive effects without typical opioid side effects, albeit it induces conditioned place preference and aversion behaviors, indicating potential for analgesic research.

Davunetide, an eight-amino-acid peptide (NAPVSIPQ), demonstrates potent neuroprotection in vitro and in vivo, enhances functional daily behaviors in schizophrenia patients, and increases memory scores in individuals with amnestic mild cognitive impairment.

SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA

U 99194 maleate (U-99194A maleate) is a D3 antagonist and increases social behaviors of isolation-induced aggressive male mice.

Varenicline Hydrochloride (CP 526555) is an orally active partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is recognized as the principal mediator of nicotine dependence, and its pharmacological effect is critical in modulating addictive behaviors associated with nicotine exposure. Varenicline Hydrochloride (CP 526555) blocks the direct agonist effects of nicotine on nicotinic acetylcholine receptors while simultaneously stimulating these receptors in a more moderate and controlled manner, making it a widely used research compound in smoking cessation.

MGS0028 is a selective agonist of metabotropic glutamate 2/3 receptor, it could reverse abnormal behaviors in mice induced by isolation rearing.

Sch 32615 is an enkephalinase inhibitor with inhibitory action on D-1 and D-2 dopamine receptor-mediated behaviors.

3'-Sialyllactose sodium is a prebiotic with anti-inflammatory activity that maintains immune homeostasis. 3'-Sialyllactose sodium reduces stressor-induced anxiety-like behaviors and can be used in studies of inflammation and arthritis.

CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in the hot plate test in mice. 1.Hahn, M., Tang, M., and Subbiah, M.T.Cholest-3,5-dien-7-one formation in peroxidized human plasma as an indicator of lipoprotein cholesterol peroxidation potentialBiochim. Biophys. Acta1255(3)341-343(1995) 2.Niu, C., Leavitt, L.S., Lin, Z., et al.Neuroactive type-A γ-aminobutyric acid receptor allosteric modulator steroids from the hypobranchial gland of marine mollusk, Conus geographusJ. Med. Chem.64(10)7033-7043(2021)

ASIC blocker (IC50 values are 0.44, 2.1 μM and no effect at rat ASIC1a, ASIC3 and ASIC2a, respectively: IC50 value = 0.12 μM at human ASIC1a with no effect at ASIC2a or ASIC3). Inhibition was also observed at heteromeric ASIC channels (IC50 values are 0.79, 0.87 and 4.5 uM at rat ASIC1a+3, ASIC1a+2a and ASIC2a+3; IC5O values are 0.33 and 0.69 uM at human ASIC1a+2a and ASIC1a+3, with no effect at ASIC2a+3). Attenuates pathophysiological nociceptive behaviors in CFA-inflamed and CCI rats.

The mating and social behaviors of insects are largely orchestrated by a suite of volatile cuticular hydrocarbon pheromones. 7(Z),11(Z)-Heptacosadiene is the predominant female-specific courtship pheromone of the fruit fly D. melanogaster. At amounts above 100 ng, 7(Z),11(Z)-heptacosadiene elicits wing vibrations in male D. melanogaster flies in a dose-dependent manner.

Scopolamine is a high-affinity (nanomolar level) muscarinic receptor antagonist that can reversibly inhibit 5-HT₃ receptor responses (IC₅₀ = 2.09 μM). It is commonly used to induce animal models of Alzheimer's disease or memory impairment.

1. Cucurbitacin IIb is one of the major active compounds in Hemsleyadine tablets which have been used for clinical treatment of bacillary dysentery, enteritis and acute tonsilitis. 2. Cucurbitacin IIb exhibits its anti-inflammatory activity through modula

IDO1/TDO-IN-4 is a novel dual inhibitor of IDO1/TDO with antidepressant activity, forming hydrogen bonds with IDO1 and π-π stacking interactions with TDO. IDO1/TDO-IN-4 rescues lipopolysaccharide-induced depressive-like behaviors in mice, used for cancer and Alzheimer's disease research.

Cinuperone is an antagonist of D2, alpha1 adrenergic and sigma receptors. The drug selectively inhibits dopamine agonists-dependent behaviors, mediated by the limbic system. The clinical development of the drug as an antipsychotic was terminated due to orthostasis.