Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
Pyridoxal phosphate-d5 (Pyridoxal 5′-phosphate-d5) is the deuterium labeled Pyridoxal phosphate. Pyridoxal phosphate is the active form of vitamin B6, acts as an inhibitor of reverse transcriptases, and is used for the treatment of tardive dyskinesia[1][2].
Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel[1][2].
Hexadecanoate-13C16 potassium is the 13C-labeled Hexadecanoate sodium. Hexadecanoate-13C16 potassium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
5-Oxoprolyltryptophan is a model substrate for investigating the increase of serotonin at the cerebral level[1].
Latanoprostene bunod (LBN), a nitric oxide (NO)-donating prostaglandin F2a analog, is a topical ophthalmic therapeutic for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension (OHT) [1].
Oxybuprocaine hydrochloride (Benoxinate hydrochloride) reversibly blocks sodium channels and prevents propagation of painful nerve impulses in the cornea, conjunctiva, and sclera. Oxybuprocaine hydrochloride is used especially in ophthalmology and otolaryngology[1][2][3].
Calcium Channel antagonist 1 is an antagonist of Calcium Channel Calcium Channel antagonist 1 has the potential for the research of neurology disease[1].
Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.Target: Histamine H1 ReceptorClemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively [1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race [2].
BRL-50481 is a novel and selective inhibitor of PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for PDE7A, PDE7B, PDE4 and PDE3, respectively.
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD)[1].
DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility[1].
CNV1014802(GSK-1014802) Hcl is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.IC50 value: Target: sodium channel blockerLike lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. CNV1014802 received orphan-drug designation from the US Food and Drug Administration in July 2013.
(+)-MK 801 Maleate is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
Parametadione (Isoethadione) is an antiepileptic agent[1].
BChE-IN-10 (compound 6) is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 6.4 μM. BChE-IN-10 can be isolated from Bletilla striata. BChE-IN-10 can be used for the research of Alzheimer's disease (AD)[1].
mHTT-IN-1 (Example 1) is a potent mutant huntingtin (mHTT) inhibitor. mHTT is toxic and a major cause of the inherited autosomal dominant neurodegenerative disorder, Huntington's disease (HD). mHTT-IN-1 conducts the reduction of mHTT with an EC50 value of 46 nM[1].
Oiligodendrocyte differentiation promoter 1 belongs to the oiligodendrocyte differentiation promoter.
Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical[1]. Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression[2].
NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM.
Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.
Orthocaine is a local anesthetic agent (extracted from patent WO2002089849A1)[1].
Flumazenil acid is a metabolite of Flumazenil[1]. Flumazenil is a GABAA receptor antagonist[2].
Biotin-myelin basic protein (94-102) is a peptide fragemt. Myelin basic protein is responsible for adhesion of the cytosolic surfaces of multilayered compact myelin, it plays an important role in the process of myelination of nerves in the nervous system. Myelin basic protein also acts as a membrane actin-binding protein, which might allow it to participate in transmission of extracellular signals to the cytoskeleton in oligodendrocytes and tight junctions in myelin[1].
FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
Pyrithioxin is a neurodynamic compound, combined with a short period of hyperventilation (HV) was applied in cerebral infarct patients with Hemiplegia.
Luciferase-IN-1 is a luciferase inhibitor[1].
CIM0216, a potent and selective agonist of TRPM3, has the ability to open two distinct cation-permeable pores in TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts as a powerful tool for use in investigating the physiological roles of TRPM3, and can be used for neurogenic inflammation research[1].