Ampalex (Ampakine CX516; CX516; BDP 12) is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator as a treatment for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI). IC50 value: Target: AMPA receptorAmpalex ameliorates functional deficits in AMPA receptors in a hippocampal slice model of protein accumulation. Researches suggest that AMPA receptors may be potential pharmaceutical targets for the treatment of neurodegenerative diseases, and highlights AMPAkines, in particular, as possible therapeutic agents.
Cipepofol-d6-2 (Ciprofol-d6-2; HSK3486-d6-2) is deuterium labeled Cipepofol (HY-116152). Cipepofol (HSK3486), a psychomotor stabilizing agent, is a gamma-aminobutyric acid (GABA) receptor potentiator.
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin[1].
(-)-N6-phenylisopropyl adenosine (D-phenylisopropyladenosine) is a adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K+-evoked Ca2+ uptake with an IC50 value of 0.5 µM[1].
LY2886721 is an BACE inhibitor used for the treatment of Alzheimer's Disease.IC50 value:Target: BACELY2886721 is a novel potent agent that is used to treat Alzheimer’s Disease in preclinical experiments. LY2886721 is under clinical study. A Safety Study of LY2886721 Multiple Doses is performing in Healthy Subjects.
Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoid receptor type 1 (CB1) with an IC50 value of 8.92 µM[1].
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
Suntinorexton, a heterocyclic compound, is an orexin type 2 receptor agonist extracted from patent WO2019027058A1, page 288[1].
Zuclopenthixol-d4((Z)-Clopenthixol-d4) succinate salt is the deuterium labeled Zuclopenthixol. Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist[1][2].
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
NSC45586 sodium is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 sodium targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 sodium can activate AKT in neurons[1].
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
BTG 1640 (ABIO-08/01) is a potent anxiolytic isoxazoline. BTG 1640 is a selective inhibitor of GABA- and glutamate-gated chloride channels[1].
SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension[1].
PIMPC is a compound with antioxidant and metal-chelating properties. PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3). PIMPC has potential anti-Alzheimer's disease effect[1].
(R)-Baclofen Hcl(STX-209 Hcl) is a derivative of gamma-aminobutyric acid (GABA) primarily used to treat spasticity and is in the early research stages for use for the treatment of alcoholism.Target: GABABaclofen (brand names Kemstro, Lioresal, Liofen, Gablofen, Beklo and Baclosan) is a derivative of gamma-aminobutyric acid (GABA). It is primarily used to treat spasticity and is in the early research stages for use for the treatment of alcoholism. It is also used by compounding pharmacies in topical pain creams as a muscle relaxant.It is an agonist for the GABAB receptors. Its beneficial effects in spasticity result from actions at spinal and supraspinal sites. Baclofen can also be used to treat hiccups, and has been shown to prevent rises in body temperature induced by the drug MDMA in rats.In addition, research has shown baclofen to be effective in the treatment of alcohol dependence and withdrawal, by inhibiting both withdrawal symptoms andcravings.
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
P2X3-IN-1 (example 7) is an inhibitor of P2X3 receptor. P2X3-IN-1 can be used for neurogenic diseases research[1].
Metaxalone-d6 is deuterium labeled Metaxalone.
Exendin-4 (3-39) is a peptide. Exendin-4 (3-39) is a truncated form of Exendin-4 (HY-13443) that lacks the first two amino acids. Exendin-4 is a potent Glucagon-like peptide-1 receptor (GLP-1r) agonist. Exendin-4 (3-39) and Exendin-4 can be used for the research of diabetic and hypothalamic-pituitary-adrenal (HPA) axis[1][2].
(R)-3-O-Methyldopa-d3 hydrochloride is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
Clomipramine HCl is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Target: 5-HT ReceptorClomipramine hydrochloride (Anafranil) is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant. Clomipramine hydrochloride (Anafranil) is a norepinephrine-reuptake inhibitor and is an antiobsessional drug. Clomipramine hydrochloride (Anafranil) is an antagonist/inverse agonist at the following receptors: D2 receptor (Ki = 162 nM), D3 receptor (Ki = 30 nM), α1-adrenergic receptor (Ki = 3.2 nM), α2-adrenergic receptor (Ki = 525 nM), H1 receptor (Ki = 31 nM), mACh receptors (Ki = 37 nM), 5-HT2A receptor (Ki = 36 nM), 5-HT2C receptor (Ki = 65 nM), 5-HT3 receptor (Ki = 85 nM), 5-HT6 receptor (Ki = 54 nM), 5-HT7 receptor (Ki = 127 nM), D1 receptor (Ki = 219 nM) [1-3].
3-Methoxyphenol is a phenolic compound that is biologically toxic. 3-Methoxyphenol is systemically absorbed, disrupts the function of the liver, kidneys, central nervous system, and redox processes, and increases levels of Hb, red blood cells, and white blood cells in the body.
NNC05-2090 (hydrochloride) is a GABA uptake inhibitor. NNC05-2090 is a betaine/GABA transporter (BGT-1) inhibitor with an IC50 value of 10.6 μM. NNC05-2090 can be used for the research of epilepsy and neurological disease[1][2].
Oxcarbazepine-D4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.IC50 value:Target: AT2 R agonistin vitro: CGP42112 (>==1 nM) significantly inhibited cGMP production from the basal value. CGP42112 (>==1 nM) significantly inhibited TH-enzyme activity from the basal value. These inhibitory effects of CGP42112 on TH-enzyme activity and-cGMP production were abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) was ineffective [1]. [125I]CGP 42112 bound selectively to the AT2 angiotensin II receptor subtype. [125I]CGP 42112 bound with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP 42112 binding in the brain, but did not alter its binding in the adrenal [2]. [125I]CGP 42112 bound with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP 42112 binding was selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP 42112 and the non-selective peptides Ang II and angiotensin III (Ang III) [4].in vivo: Intravenous infusions of CGP 42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF [3].
NT-0796 is a selective and CNS-penetrant NLRP3 inflammasome inhibitor with an IC50 of 0.32 nM in PBMC assay. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 has the potential for neuroinflammatory diseases research[1].
Nemorexant is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.
OX2R-IN-1 is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 can cross the BBB into the brain with a short half-life[1].
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA)[1].