Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion[1].
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.IC50 Value: Target: GABA receptorin vitro: AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1]. in vivo: AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3].
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases[1][2].
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine[1].
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
Galantide is a reversible and non-specific galanin receptor antagonist.
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect[1][2].
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation[1].
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].
Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.
(Z)-Hexadec-9-enoic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD)[1].
Blonanserin(AD-5423) is a D2/5-HT2 receptor antagonist, atypical antipsychotic. Target: D2 receptor; 5-HT2 receptorBlonanserin(AD-5423) is a relatively new atypical antipsychotic for the treatment of schizophrenia. Blonanserin belongs to a series of 4-phenyl-2-(1-piperazinyl)pyridines and acts as an antagonist at dopamine D2, D3, and serotonin 5-HT2A receptors. Blonanserin has low affinity for 5-HT2C, adrenergic α1, histamine H1, and muscarinic M1 receptors, but displays relatively high affinity for 5-HT6 receptors [1]. AD-5423 bound preferentially to dopamine (DA)-D2 (Ki, 14.8 nM; cf. haloperidol, 8.79 nM; and clozapine, 149 nM) and serotonin (5-HT)-S2 (Ki, 3.98 nM; cf. haloperidol, 26.8 nM; and clozapine, 8.66 nM) receptors. It displayed low affinity for adrenaline (Ad)-alpha-1 (Ki, 56.3 nM) receptors and was virtually devoid of binding to DA-D1 (Ki, 2870 nM), 5-HT-S3, Ad-alpha-2, Ad-beta, muscarine, tau-aminobutyric acid and benzodiazepine receptors. In addition, AD-5423 was only a weak inhibitor of DA, 5-HT and noradrenaline uptake systems. AD-5423 (0.2-2 mg/kg p.o.) decreased exploratory activity in mice. AD-5423 (10 mg/kg p.o.), unlike haloperidol, did not antagonize SKF38393-induced vacuous oral movements in rats. Head twitches induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane in mice and by para-chloroamphetamine in rats were antagonized by AD-5423 at much lower doses (0.5-2 mg/kg p.o.) than those of haloperidol and clozapine [2].
PBB3, a selective PET ligand, recognizes tau pathology in Alzheimer's disease brains, where dystrophic neurites and diffuse neurofibrils are more clearly detected Tangles with calcification[1].
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
Duoperone is a neuroleptic agent and also a antiemetic agent in animal models.
MK-7622 is a muscarinic M1 receptor positive allosteric modulator.Target: M1 receptorMK-7622 is useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders.
rel-Quinpirole (rel-LY 141865) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases[1].
Argipressin (Arg8-vasopressin) (acetate) binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a Kd value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1[1][2][3][4].
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM)[1].
Cardioexcitatory peptide 1 is a cardioexcitatory neuropeptide, can be isolated from Achatina atria. Cardioexcitatory peptide 1 has potent cardio-excitatory action on the hearts and also modifies the motility of muscular tissues and neural activities[1].
SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.IC50 value: 8.0 (pKi)Target: D3 receptor
Cyclohexanecarboxylic acid-d1 is the deuterium labeled Cyclohexanecarboxylic acid[1]. Cyclohexanecarboxylic acid is a Valproate structural analogue with anticonvulsant action[2].
NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research[1].
Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation[1][2].
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research[1].
(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].
Neoechinulin C, an echinulin-related indolediketopiperazine alkaloid, protects the neuronal cells against paraquat-induced damage in a Parkinson’s disease model[1].
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].