Decaffeoylacteoside is an inhibitor of AChE/BChE/LOX with moderate activity[1].
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively[1].
Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex[1][2].
JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
CGP11952 is a triazolyl-Benzaphenon resembling the benzodiazepines in its pharmacological action. CGP11952 is an experimental benzodiazepine derivative.
CL-275838 is a memory-enhancing agent, also with potent antidepressant activities.
Domperidone-d6 (R33812-d6) is the deuterium labeled Domperidone. Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1][2].
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
Eicosapentaenoic acid (EPA) is an omega-3 fatty acid.
Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].
N-Methyldopamine hydrochloride is a precursor of adrenaline in the adrenal medulla. N-Methyldopamine hydrochloride is a modification of the dopamine (DA), and retains agonist activity at the DA1 receptor. N-Methyldopamine hydrochloride remains capable of universal surface coating and secondary reactions using the surface catechols. N-Methyldopamine hydrochloride can be used for heart failure research[1][2][3].
THX-B is a potent and non-peptidic p75NTR (neurotrophin receptor p75) antagonist. THX-B can be used in the research of diabetic kidney disease, neurodegenerative and inflammatory disorders[1][2][3].
GpTx-1 is a potent, selective, 34-residue peptide antagonist of Nav1.7 sodium channel with IC50 of 10 nM, displays 20- and 1000- fold selectivity over NaV1.4 and NaV1.5.
W-2429 is a non-narcotic analgesic agent.
Suavissimoside R1, isolated from the roots of Rubus parvifollus, possesses potent neuroprotective activity and has the potential to treat anti-Parkinson's disease drug[1].
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
Oxotremorine sesquifumarate is a mAChR agonist that mainly activates M2 receptors. Oxotremorine sesquifumarate can be used for neurological research[1][2].
Pergolide (LY127809 (free base)) is an ergot-derived orally active dopamine receptor agonist. Pergolide can be used for Parkinson disease research[1].
Ciramadol (WY 15705) is a potent and orally active analgesic agent with both narcotic agonist and antagonist properties[1]. Ciramadol (WY 15705) can be used for postoperative pain treatment research.
Atomoxetine Hcl(LY 139603; Tomoxetine Hcl) is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively). IC50 value: 5 nM (Ki for human NET)Target: NETAtomoxetine displays minimal affinity for a range of other neurotransmitter receptors and transporters (Ki > 1 μM). Atomoxetine is antidepressant and a commonly used non-stimulant treatment for Attention deficit hyperactivity disorder (ADHD).
(Gly22)-Amyloid β-Protein (1-42) is a peptide fragment of amyloid β-protein (Aβ). Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease. Mutation of Glu22 to Gly22 in Aβ can increase aggregation[1][2].
PF-592379 is a potent dopamine D3 receptor agonist with an EC50 of 21 nM.
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
PG01037 (dihydrochloride) is a potent and selective dopamine D3 receptor antagonist with a Ki of 0.7 nM[1].
Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.
Cytidine-13C-1 is the 13C labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholami
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD)[1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM[2].
Levetiracetam(UCB L059) is a novel anticonvulsant with antihyperalgesic efficacy in inflammatory pain.Target: Calcium ChannelLevetiracetam is used to control some types of seizures in patients with epilepsy. This medicine cannot cure epilepsy and will only work to control seizures for as long as you continue to use it. The exact mechanism for levetiracetam is unknown. However, the drug binds to a synaptic vesicle protein, SV2A, which is believed to impede nerve conduction across synapses [1].Levetiracetam (10-200 mg/kg), ibuprofen (12.5-100 mg/kg), celecoxib (3.75-30 mg/kg), paracetamol (50-200 mg/kg), caffeine (15-100 mg/kg), and 2-drug combinations of levetiracetam with analgesics/caffeine produced a significant, dose-dependent reduction of inflammatory hyperalgesia. Isobolographic analysis revealed that levetiracetam exerts a synergistic interaction with analgesics, with approximately 7-, 9-, and 11-fold reduction of doses of both drugs in combination of levetiracetam with paracetamol, celecoxib, and ibuprofen, respectively. Analysis of the log dose-response curves for levetiracetam (1-50 mg/kg) in the presence of caffeine (10 mg/kg) and levetiracetam applied alone also revealed a synergistic interaction. Levetiracetam's ED50 in the presence of caffeine was reduced approximately 11-fold [2].Clinical indications: Epilepsy; Social phobiaFDA Approved Date: November 2008Toxicity: depression; hallucinations; suicidal thoughts
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research[1][2][3].