behaviors

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

Neuropeptide S (Mouse) acetate is a bioactive peptide. Neuropeptide S (Mouse) acetate, as a neurotransmitter/neuromodulator of 20 amino acids, can be used for the research of arousal, anxiety, locomotion, feeding behaviors, memory and drug addiction[1].

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

TAT-P4-(DATC5)2 TFA, a high-affinity peptide inhibitor targeting the PDZ domain of protein interacting with C kinase-1 (PICK1), exhibits a K i of 1.7 nM and demonstrates potential in mitigating addiction behaviors in rats [1].

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

TNO211 is a bioactive peptide that functions as a highly soluble fluorogenic substrate for select Matrix Metalloproteinases (MMPs)—specifically MMP-2, 8, 12, 13, and 14. Incorporating a cleavable Gly-Leu bond and an EDANS/DABCYL fluorophore/quencher pair, TNO211 enables sensitive detection of MMP activity through fluorescence assays, with an absorption/emission profile at 340/490 nm. It is particularly effective in analyzing MMPs in culture media from endothelial cells as well as untreated synovial fluid from patients, highlighting its utility in investigations of MMP-associated cellular behaviors, including proliferation, migration (adhesion/dispersion), differentiation, angiogenesis, apoptosis, and host defense.

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.

Utatrectinib (AZD-7451) is a potent, orally active, and selective Trk inhibitor that effectively inhibits TrkC activation and associated tumorigenic 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.

Desethoxy quetiapine, an active metabolite of the atypical antipsychotic quetiapine, primarily forms through the action of the cytochrome P450 (CYP) isoform CYP3A5. This compound binds to dopamine D2 receptors with an IC50 value of 1,330 nM. In vivo, desethoxy quetiapine at dosages of 20 and 40 mg/kg mitigates dopamine receptor agonist apomorphine-induced climbing behavior and ameliorates swimming deficits in mice, showcasing its potential modulatory effects on dopamine-mediated behaviors.

The compound 4A7C-301-Nurr1 agonist is a specific agonist for the nuclear receptor-related 1 (Nurr1). By binding to the Nurr1 ligand-binding domain with an IC50 value of 48.22 nM, it enhances the transcriptional activity of both Nurr1-LBD and the full-length Nurr1, as demonstrated in reporter assays using SK-N-BE(2)C human neuroblastoma cells, with EC50 values of 6.53 and 50-70 µM, respectively. Additionally, administration of 4A7C-301-Nurr1 agonist at a dosage of 5 mg/kg per day has been shown to mitigate dopaminergic cell death in the striatum and substantia nigra pars compacta and ameliorate motor and olfactory deficits in mouse models of Parkinson's disease, circumventing the induction of dyskinesia-like behaviors. These models were induced either by the neurotoxin MPTP or by overexpression of α-synuclein.

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

[Des-Tyr1]-gamma-Endorphin is a neuropeptide found in human cerebrospinal fluid. It exhibits antidepressant activity, helps eliminate active avoidance behaviors in rats, and reduces passive avoidance behaviors in these animals.

Compound 4h, also known as 5-HT7R antagonist 2, is a selective inhibitor of the 5-HT7R that disrupts both G protein and β-arrestin signaling pathways. It exhibits a K_i value of 67 nM, with IC_50 values of 2.59 μM in cAMP assays and 39.57 μM in Tango tests. This antagonist is noted for its potential to mitigate repetitive behaviors associated with autism spectrum disorder (ASD) and to foster the restoration of neurogenesis impaired by ASD [1]. Pharmacokinetic analysis in ICR male mice following intravenous and intraperitoneal administration shows a T_max of 0.08 hours and 0.25 hours, a T_1 2 of 0.77 hours and 1.06 hours, and a C_max of 33.07 ng mL and 156.44 ng mL, respectively. The AUC_last was recorded at 28.31 ng·h mL and 143.27 ng·h mL, with a clearance rate (CL) of 41.61 L h kg for intravenous administration. The volume of distribution at steady state (V_ss) was 32.43 L kg, the mean residence time (MRT) was 0.79 hours and 0.93 hours, and the bioavailability (F) was calculated at 50.60% [1].

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

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.

VUAA1, an insect odorant co-receptor (Orco) agonist, activates heteromeric and homomeric Orco-containing channels and can disrupt the behaviors of nuisance insects, thus serving as a tool for insect olfactory research [1] [2].

TAT-P4-(DATC5)2 is a potent peptide inhibitor of the PDZ domain of protein interacting with C kinase-1 (PICK1), with a high affinity dissociation constant (K_i) of 1.7 nM. This compound has demonstrated the ability to mitigate addiction behaviors in rat models [1].

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.

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)

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.

CART (1-39), Human, Rat is a neuropeptide comprising the first 39 residues of the CART peptide. This compound acts as a rat satiety factor with significant appetite-suppressing effects and is closely associated with leptin and neuropeptide Y. It inhibits regular and starvation-induced feeding and can induce anxiety and stress-related behaviors [1].

OPC 4392 hydrochloride acts as an agonist at presynaptic dopamine receptors (dopamine receptor) and as an antagonist at postsynaptic D2 receptors. It reverses dopamine accumulation induced by Reserpine and inhibits stereotyped and climbing behaviors in a mouse model induced by Apomorphine.

Valerena-4,7(11)-diene, a tranquilizer, suppresses stress-induced excitatory behaviors and is administered through olfactory stimulation and pulmonary absorption [1].

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].

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

Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.