HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research[1].
Novel fluorescent substrate for both the serotonin transporter and the vesicular monoamine transporter 2 (VMAT2)
(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms[1][2].
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].
(RS)-MCPG is a non-selective group I/group II metabotropic glutamate receptor antagonist.
Thiamine monochloride (Vitamin B1) is an essential vitamin that plays an important role in cellular production of energy from ingested food and enhances normal neuronal actives.
Carbamazepine-d8 is the deuterium labeled Carbamazepine. Carbamazepine, a sodium channel blocker, is an anticonvulsant drug, with an IC50 of 131 μM[1][2].
5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 free base has antipsychotic drug-like activity. 5-HT2C agonist-3 free base blocks Amphetamine-induced hyperactivity[1].
Eperisone-d10 ((±)-Eperisone-d10) hydrochloride is the deuterium labeled Eperisone hydrochloride. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an antispastic agent used for treatment of diseases characterized by muscle stiffness and pain. It works by relaxing both skeletal muscles and vascularsmooth muscles, thus demonstrating avariety of effects such as reduction ofmyotonia, improvement of circulationand suppression of the pain reflex. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is a centrally acting muscle relaxant inhibiting the pain reflex pathway, having a vasodilator effect[1][2 [3].
C-DIM12 is a synthetic Nurr1 activaor induces Nurr1 and DA gene expression in cell lines and primary neurons.Target: Nurr1in vitro: C-DIM12 as a modulator of Nurr1 activity that results in inhibition of NF-κB-dependent gene expression in glial cells by stabilizing nuclear corepressor proteins, which reduces binding of p65 to inflammatory gene promoters. C-DIM12 Decreases Inflammatory Gene Expression in BV-2 Microglia. C-DIM12 Decreases Expression of NF-κB-Enhanced GFP Expression in Human Embryonic Kidney 293 Reporter Cells.[1] C-DIM12 increases protein levels of exogenously expressed human Nurr1 in transfected neurons.C-DIM12 protects neurons from 6-hydroxydopamine toxicity. [2]
Arbaclofen placarbil is a novel transported prodrug of the active R-isomer of baclofen. Baclofen is a racemic GABAB receptor agonist
Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels[1].
α-Conotoxin MrIC is an α7nAChR biased agonist. α-Conotoxin MrIC exclusively activates α7nAChR regulated by type II positive allosteric modulators, including PNU120596. α-Conotoxin MrIC can be used to study neurological diseases and also to probe the pharmacological properties of α7nAChR[1].
AChE/BChE-IN-2 (Compound 13b) is a potent inhibitor of AChE/BChE (AChE IC50 = 0.96 ± 0.14 µM, BChE IC50 = 1.23 ± 0.23 µM). AChE/BChE-IN-2 has the potential for the research of AD diseases[1].
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects[1][2].
T3D 959 (DB-959) is a potent, brain penetrant, orally active dual PPARδ/PPARγ agonist with EC50 of 19/297 nM, respectively; prevents STZ-induced neurotoxicity, and shows clear therapeutic and neuroprotective effects in an established model of sporadic AD. Alzheimer Disease Phase 2 Clinical
Xylazine Hydrochloride is α2 class of adrenergic receptor agonist.Target: Adrenergic ReceptorXylazine is a drug that is used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle and other non-human mammals. An analogue of clonidine, it is an agonist at the α2 class of adrenergic receptor. Xylazine has recently emerged as a recreational drug, especially in Puerto Rico [1]. Administration of xylazine (0.17 mg/kg of body weight, diluted to a 10-ml volume, using 0.9% NaCl) induced approximately 2.5 hours of local analgesia without apparent side effects. Higher doses of xylazine caused mild hind limb ataxia. Administration of lidocaine induced a similar duration of analgesia, with severe hind limb ataxia (100% incidence). We concluded that xylazine given by epidural injection results in safe, effective perineal analgesia in horses [2].
Isoatriplicolide tiglate is a bioactive sesquiterpene lactone. Isoatriplicolide tiglate can be isolated from Paulownia coreana. Isoatriplicolide tiglate has neuroprotective effect[1].
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].
DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect[1][2][3].
Lintopride is a 5HT4 antagonist with moderate 5HT3 antagonist properties.
Methyl ganoderate A acetonide, a lanostane triterpene, is a natural product that could be isolated from the fruiting bodies of Ganoderma lucidum. Methyl ganoderate A acetonide is a potent AChE inhibitor with an IC50 value of 18.35 μM. Methyl ganoderate A acetonide can be used in research of Alzheimer’s disease (AD)[1].
Harmaline is a potent and reversible monoamine oxidase inhibitor in vivo. Harmaline is a central nervous system stimulant and can be used to induce tremor in rodents.
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[1]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[2].
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures[1].
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells[1][2][3].
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia[1][2].
ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
Dimenhydrinate is an anti-emetic and anti-histamine commonly available over-the-counter as a motion sickness remedy.