Lazabemide(Ro 19-6327/000) is selective, reversible monoamine oxidase B (MAO-B) inhibitor (IC50 values are 0.03 and > 100 μM for MAO-B and MAO-A respectively).IC50 value: 30 nM [1]Target: MAO-B inhibitorin vitro: The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmax values for 3H-Ro 41-1049 in rat cerebral cortex were 10.7 nM and 7.38 pmol/mg protein, respectively, and for 3H-Ro 19-6327 were 18.4 nM and 3.45 pmol/mg protein, respectively [1]. The IC50 values for lazabemide and Ro 16-6491, respectively, were: 86 microM and 90 microM for NA uptake; 123 microM and 90 microM for 5HT uptake; > 500 microM and > 1000 microM for DA uptake. Lazabemide and Ro 16-6491 also differed from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Ro 16-6491 (500 microM) induced a greater 5 HT release than did L-deprenyl, but was less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release [2]. a clear inhibition of DOPAC formation was observed with Ro 41-1049 (250 nM), while 250 nM lazabemide was found not to increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA [3].in vivo: The ischemia reperfusion-induced hydroxyl radical generation was attenuated by 3 mg/kg of clorgyline and lazabemide. Furthermore, mice pretreated with these MAO inhibitors showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups; recovery of the reduced DOPAC level was also delayed [4].
Ralfinamide (FCE-26742A) is an orally available Na(+) channel blocker derived from α-aminoamide, with function of suppressing pain[1].
BW373U86 (SNC86) is a δ-opioid receptor agonist with an IC50 of 1.49 nM. BW373U86 shows antidepressant-like effects[1].
CLP290 is an orally available activator of the neuron-specific K+-Cl− cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats[1][2].
[Arg-15,-20,-21,Leu17]-PACAP-Gly-Lys-Arg-NH2 (BM-PACAP) is a synthetic PACAP 1-27 (HY-P0176) analogue with relaxant effect[1].
LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo[1].
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury[1][2].
H-Phe-Phe-OH is a peptide made of two phenylalanine molecules; Phenylalanine is an essential amino acid and the precursor for the amino acid tyrosine.
SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities[1].
8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site[1].
Zicronapine is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors.
Dihydrexidine (DAR-100) is a high potent, selective and full efficacy D1 dopamine receptor agonist with an IC50 of 10 nM, and displays some affinity for the D2 receptor. Dihydrexidine (DAR-100) exhibits potent antiparkinsonian activity[1][2][3].
Ubretid is a potent inhibitor of plasma cholinesterase. Ubretid therefore delays the hydrolysis of suxamethonium and prolongs its action, similar to the effects shown by other anticholinesterase drugs, such as pyridostigmine and donepezil. Ubretid has the potential for the research of urinary retention prolongs the effect of suxamethonium. Ubretid is commonly prescribed for the research of myasthenia gravis and for difficulty in emptying the bladder[1].
(+)-Phenserine is a novel selective cholinesterase noncompetitive inhibitor with an IC50 of 45.3 μM.
PF-06795071 is a potent and selective covalent MAGL inhibitor with an IC50 of 3 nM[1].
Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition[1].
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist. Target: NMDARapastinel is a robust cognitive enhancer and facilitates hippocampal long-term potentiation (LTP) of synaptic transmission in slices.
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease[1].
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52[1].
Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM.
5-HT2A receptor agonist-1 is a 5-HT2A receptor agonist with the EC50 of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders[1].
Butabindide (UCL-1397) oxalate is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide oxalate inhibits TPP II to protect CCK-8 against inactivation[1][2].
L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects[1].
(S)-GFB-12811 (compound 596) is a potent and selective CDK5 inhibitor, with an IC50 value less than 10 nM. (S)-GFB-12811 can be used in the research of cell cycle progression, neuronal development, tumorigenesis[1].
3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of GABA, is a GABAB receptor agonist[1].
Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects[1][2][3].