A potent, subtype-selective α3β4 nAChR partial agonist with Ki of 0.62 nM; selectively activates receptors containing β4- but not β2-subunits, shows no efficacy at α4β2 receptors and only marginal efficacy at α4β4 receptors expressed in oocytes; enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment.
Rolziracetam is a nootropic drug of the racetam family and improves short-term memory in rats and monkeys[1].
STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection[1].
Dihydrolycorine is isolated from Lycoris radiate Herb with antihypertensive and neuroprotective activities[1]. Dihydrolycorine is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step[2].
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors[1][2][3].
TKIM is a TREK-1 channel inhibitor with an IC50 of 2.96 μM. TKIM binds to the pocket of the intermediate (IM) state of TREK-1[1].
CAY10404 is a potent and highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM. CAY10404 exhibits no inhibition of COX-1 (IC50>500 µM)[1]. CAY10404 is a potent inhibitor of PKB/Akt and MAPK signaling pathways and induces apoptosis in NSCLC cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities[2][3].
Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity[1].
ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research[1].
ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Bromisoval has anti-inflammatory effects and has been used as an old sedative and hypnotic.
Ozanezumab (GSK1223249) is an anti-Nogo-A (neurite outgrowth inhibitor A) monoclonal antibody. Ozanezumab can be used in amyotrophic lateral sclerosis (ALS) and multiple sclerosis research[1].
Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.IC50 value: 0.82 nM/3.14 nM (5-HT1B/5-HT1D, Ki) [1]Target: 5-HT1B/5-HT1D in vitro: [3H]Eletriptan has a total number of binding sites (Bmax) of 2478 fmol/mg and 1576 fmol/mg for 5-HT1B and 5-HT1D, respectively. [3H]Eletriptan has a significantly faster association rate (K(on) 0.249/min/nM) than [3H]sumatriptan (K(on) 0.024/min/nM) and a significantly slower off-rate (K(off) 0.027/min compared to 0.037/min for [3H]sumatriptan) [1]. Eletriptan induces concentration-dependent contractions of meningeal artery, coronary artery, and saphenous vein. The potency of Eletriptan is higher in meningeal artery than in coronary artery (86-fold) or saphenous vein (66-fold). The predicted contraction by Eletriptan (40 mg and 80 mg) and sumatriptan (100 mg) at free C(max) observed in clinical trials is similar in meningeal artery [2].in vivo: Eletriptan (<1000 mg/kg, i.v.) produces a dose-dependent reduction of carotid arterial blood flow in the anaesthetised dog. Eletriptan reduces coronary artery diameter with ED50 value of 63 mg/kg in the anaesthetised dog. Eletriptan (<300 mg/kg, i.v.) administered prior to electrical stimulation of the trigeminal ganglion produces a dose-related and complete inhibition of plasma protein extravasation in the dura mater rats. Eletriptan (100 mg/kg, i.v.) produces a complete inhibition of plasma protein extravasation in rat dura mater [3]. Iontophoretic ejection (50 nA) of Eletriptan suppresses the response in 75% of cells and causes an average suppression of cell firing of 42% in cats [4].
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4].
Ovotransferrin (328-332) has a protective activity on the blood pressure by inhibiting the Angiotensin-Converting Enzyme (ACE), with the IC50 of 20 μM. Ovotransferrin (328-332) fragment has an activity against Cholinesterase (ChE), implicating in Alzheimer’s diseases[1][2].
Palmitic acid-13C is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface[1].
3-AQC, a piperazinylquinoxaline derivative, is a potent and competitive 5-HT3 receptor antagonist[1].
Folic acid (Vitamin B9) sodium is a orally active essential nutrient from the B complex group of vitamins. Folic acid sodium shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid sodium can be used to the treatment of megaloblastic and macrocytic anemias due to folic deficiency[1][2][3][4].
JNJ-55511118 (JNJ55511118) is a selective, orally available AMPA receptor containing TARP-γ8 negative modulator with Ki of 26 nM, displays no significant activity against other TARP-less AMPARs and AMPARs coexpressed with other TARPs or CNIH2; demonstrates excellent pharmacokinetic properties and achieves high receptor occupancy following oral administration, exhibits a strong reduction in certain bands on electroencephalogram, transient hyperlocomotion, no motor impairment on rotarod, and a mild impairment in learning and memory in vivo.
CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2[1].
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD)[1].
Nivasorexant is a potent orexin receptor antagonist[1].
DSPE-NHS is a bioconjugation phospholipid molecule with two hydrophobic lipid tails. DSPE-NHS is a self-assembling reagent which forms lipid bilayer in aqueous solution. DSPE-NHS can be used to prepare liposomes as drug nanocarrier[1].
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease[1][2][3].
Paeonilactone B is a monoterpene with neuroprotective effect against oxidative stress. Paeonilactone B protects rat cortical cells against H2O2-induced neurotoxicity[1].
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].
ω-Conotoxin CVID (Leconotide, AM336, CNSB004) blocks neuronal voltage sensitive calcium channel[1].
Velufenacin is a muscarinic receptor antagonist[1].