Ozanimod (hydrochloride) (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod (hydrochloride) (RPC-1063) has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod (hydrochloride) (RPC-1063) can be used for the research of relapsing multiple sclerosis (MS) [1].
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor[1].
P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats[1].
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].
Shinjulactone M is a quassinoid isolated from various parts of Ailanthus species. Ailanthus, an important genus of the Simaroubaceae family, can be used as an febrifuge (antimalarial) and anthelmintic, and is given for the research of chronic bronchitis, epilepsy and asthma[1].
DCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects[1][2].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
Guattegaumerine is a bisbenzylisoquinoline alkaloid with antimitotic, cytotoxic and neuroprotective activities[1].
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively[1].
VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM[1].
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research[1][2].
Tetramethylglycerol (Tetramethylglycoluril) is a small molecule that acts on GABA Receptor, with anti-anxiety activity[1].
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake[1][2].
A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM; significantly reduces depositions of Aβ3(pGlu)-40/42 in brain in transgenic mouse models and Drosophila model of Alzheimer diseas.
OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing[1].
Pi-Methylimidazoleacetic acid hydrochloride is a potential neurotoxin[1].
A small-molecule inhibitor of STOML3 oligomerization that reverses pathological mechanical hypersensitivity in vivo; effectively inhibits the self-association of stomatin, STOML1 and STOML2 at 2 uM, but not podocin; reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo; also reversibly attenuates fine touch perception in normal mice, reverses pathological mechanical hypersensitivity.
PACAP-38 (16-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production[1]. PACAP is a potent activator of cAMP formation[2].
Verdiperstat (AZD3241) is a selective, irreversible and orally active myeloperoxidase inhibitor, with an IC50 of 630 nM, and can be used in the research of neurodegenerative brain disorders.
Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in clinical[1][2].
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil acts on the vascular system and the heart and nodal structure[1]. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM[2].
2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research[2].
Aripiprazole(Abilify) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. IC50 Value: 4.2 nM(Ki)Target: 5-HT ReceptorAripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors.
Carbromal (Adalin; Adisomnol) is a sedative with centrally depressant effects[1].
Desoxypeganine (Deoxypeganine), an alkaloid, is a potent and orally active cholinesterase (BChE and AChE) and selective MAO-A inhibitor, with IC50 values of 2, 17, and 2 μM, respectively. Desoxypeganine can be used for alcohol abuse research[1].
KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate and has antiepileptic effect[1].
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease[1][2].