(±)-Acetylcarnitine chloride (Acetyl dl-carnitine chloride) is a weak cholinergic agonist with cholinergic properties. (±)-Acetylcarnitine chloride is an important intermediate in lipid metabolism[1][2].
RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017.
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV)[1][2].
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis[1].PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
Reboxetine Mesylate is a norepinephrine reuptake inhibitor use in the treatment of unipolar depression.Target: OthersReboxetine is a drug of the norepinephrine reuptake inhibitor class. Reboxetine dose-dependently and potently inhibits locus coeruleus neuronal firing in rats with ED50 of 191 μg/kg. Reboxetine inhibition of the locus coeruleus neurons is reversible by the α2 antagonist piperoxan (1.5 mg/kg, IV). Reboxetine dose-dependently reverses reserpine-induced blepharospasm and hypothermia in the mouse. Reboxetine is also found to antagonize clonidine-induced hypothermia dose-dependently in mice. Reboxetine reverses reserpine-induced blepharospasm and hypothermia in rats with ED50 of 10 mg/kg and 3 mg/kg (p.o.), respectively [1]. Reboxetine is associated with a markedly lower relapse rate than placebo (22% vs. 56%) and a greater cumulative probability of a maintained response during long-term treatment in patients with recurrent DSM-III-R major depression. Reboxetine effectively prevents recurrence of depressive symptoms following episode resolution [2]. Acute systemic administration of Reboxetine (0.3 mg/kg-20 mg/kg) dose-dependently increases extracellular norepinephrine in the rat frontal cortex while having no effect on extracellular serotonin. Reboxetine (20 mg/kg) also increases extracellular dopamine in the rat frontal cortex. Chronic administration of Reboxetine for 14 days results in elevated basal concentrations of extracellular norepinephrine and dopamine and a greater net increase of extracellular norepinephrine and dopamine, but not serotonin in the rat frontal cortex [3].
LSP4–2022 is a novel potent, selective, brain-penetrant mGluR4 agonist with EC50 of 0.11 uM in cell-based assays; displays >100-fold selectivity over mGlu7 and mGlu8 (IC50=11.6 and 29.2 uM), no activity at the group I and -II mGlu receptors (EC50>100 uM); inhibits neurotransmission in cerebellar slices from mice, and possesses antiparkinsonian properties in a haloperidol-induced catalepsy test.
Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders[1][2].
Drinidene can be used for the research of pain disorders extracted from patent AU2018254530A1[1].
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
Crassicauline A (Crassicaulin A) is a bioactive alkaloid found in roots of Aconitum carmichaeli. Crassicauline A (Crassicaulin A) possesses feeding deterrent activity against T. castaneum adults with an EC50 of 1134.5 ppm[1][2].
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for the treatment of schizophrenia[1].
Salirepin is a phenolic glycoside from fruits of Idesia polycarpa, inhibits LPS-induced nitric oxide production[1].
Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research[1][2][3].
Colivelin is a neuroprotective peptide and activator of STAT3.
β-Amyloid (1-40), FAM-labeled is a FAM fluorescently-labelled β-Amyloid (1-40) peptide (λex= 492 nm and λem= 518 nm)[1].
Effusol, a phenolic constituent from Juncus effuses, exhibits potent scavenging activity for DPPH and ABTS radicals, with IC50 values of 79 μM and 2.73 μM, respectively. Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline[1].
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect[1].
Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity[1][2].
(+)-Menthol (D-Menthol) is one of the optical isomers of Menthol. (+)-Menthol can reduce the electrically evoked contractions of rat phrenic hemidiaphragm in vitro. Local anaesthetic activity. (+)-Menthol can also inhibit the growth of Microcystis aeruginosa cells[1][2][3].
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation[1]. 1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity[2].
Arcaine (sulfate) is a glutamate NMDA receptor inhibitor[1].
Nefopam-d4 (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Nefazodone hydrochloride is an antidepressant drug.
Magnolioside, isolated from Angelica gigas Nakai (Umbelliferae), exhibits significant neuroprotective activities against glutamate-induced toxicity[1].
Talatisamine, a aconitum alkaloid，is specific K+ channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons[1].
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation[1].
SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression[1][2][3][4].
Atropine is a medication used to treat certain types of nerve agent and pesticide poisonings, some types of slow heart rate, and to decrease saliva production during surgery.