AM1241 is a potent, typical[2] and selective CB2 receptor agonist, with a Ki of 3.4 nM in a mouse spleen, and the Ki for CB1 receptor in rat brain is 280 nM, 82-fold selectivity for the CB2 receptor in rodent tissue[1]. AM1241 relieves migraine, stroke, and neuropathic pain，also has a potent effect on Parkinson's disease[2]. AM1241 prevents oxidative damage and activates STAT3 through the phosphorylation of Akt and Erk1/2[3].
Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease[1].
ABC44 is a potent serine hydrolase inhibitor with IC50s of 0.1 μM and 6.5 μM for palmitoyl protein thioesterase 1 (PPT1) in situ and in vitro, respectively. ABC44 can be used for researching infantile neuronal ceroid lipofuscinosis[1].
JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].
GSK1059865 is a potent orexin 1 receptor antagonist.
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[1][2][3][4].
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB[1].
Valepotriate, isolated from Valeriana jatamansi Jones, has anti-epileptic and anti-cancer activities[1][2].
BIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively[1].
BACE1-IN-6 is a BACE1 inhibitor with an IC50 value of 1.5 nM.
Curculigoside C is a phenolic glucoside with potent antioxidative and neuroprotective activities. Curculigoside C shows IC50 values of 0.25 mM and 0.88 mM for hydroxyl radicals and superoxide anion radicals, respectively[1].
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease[1].
Tolperisone is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.
SCH-23390-d3 (R-(+)-SCH-23390-d3) hydrochloride is the deuterium labeled SCH-23390 hydrochloride. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM[1][2][3].
Fentonium bromide is an anti-ulcerogenic, anticholinergic and antispasmodic agent. Fentonium bromide can be used in the research of neurological conditions[1][2][3].
α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential[1].
Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.Target: 5-HT1 agonist Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches. It is believed to work by narrowing the blood vessels around the brain. Rizatriptan also reduces the substances in the body, which can also reduce headache pain, nausea, sensitivity to light and sound and other migraine symptoms.Rizatriptan was rapidly absorbed with a median tmax of 1.3 h (range 1-3 h) vs a tmax for sumatriptan of 2.5 h (range 1-4 h, P < 0.001). Administration of either rizatriptan or sumatriptan produced maximal mean elevations of 5-10 mmHg in systolic and diastolic blood pressures without effect on heart rate; the changes occurred sooner following rizatriptan, consistent with more rapid absorption. Both rizatriptan and sumatriptan provoked mild increases in serum growth hormone without any effect on serum prolactin concentrations. The most commonly reported symptom following rizatriptan was drowsiness.
gamma-secretase modulator 3 is a gamma-secretase modulator.
D-Galactose-d2-1 is the deuterium labeled D-Galactose. D-Galactose is a natural aldohexose and C-4 epimer of glucose.
Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM[1].5-O-Demethylnobiletin (5-demethylnobiletin) promotes neuritogenesis through the activation of MAPK/ERK-, PKC-, and PKA-dependent signaling pathways[2].
Dioxone is a substance possessing convulsant properties qualitatively similar to leptazol and bemegride. Dioxone is orally active[1].
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats[1].
1-Aminocyclobutanecarboxylic acid is a NMDA receptor partial agonist acting at the glycine site, NR1[1].
Dehydrogeijerin is an inhibitor of acetylcholinesterase with an IC50 of 9.7 μM. Dehydrogeijerin can be used in study Alzheimer’s disease[1].
(±)-5'-Chloro-5'-deoxy-ENBA is an agonist of A1AR. (±)-5'-Chloro-5'-deoxy-ENBA produces hypothermia in mice[1].
Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.