Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].
D-Galactose-13C,d1 is the deuterium and 13C labeled D-Galactose. D-Galactose is a natural aldohexose and C-4 epimer of glucose.
WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex[1]. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects[2].
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Nav1.1 channels positive modulator. Lu AE98134 also increases the activity of Nav1.2 and Nav1.5 channels but not of Nav1.4, Nav1.6 and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].
MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95). MIPS521 exhibits pain-relieving effects in vivo[1][2].
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain[1].
Udonitrectag (REC 0559), a low molecular weight compound that mimics NGF, aims to address the issue of NGF stability[1].
Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC)[1][2].
Fluzinamide is an effective antiepileptic.
Donepezil Hcl(E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine. IC50 Value:Target: AChEIt is known that Donepezil Hydrochloride is a useful tool in the study of Alzheimer's disease. Studies indicate that Donepezil Hydrochloride protects the brain against diisopropylfluorophosphate-induced effects. Studies indicate that Donepezil Hydrochloride selectively inhibits acetylcholinesterase, whereas it has little effect on butyrylcholinesterase. Alternate studies suggest that Donepezil Hydrochloride increases the concentration of extracellular acetylcholine in the cerebral cortex and hippocampus of rats.
RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
Etifoxine-d3 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
ASS234 (ASS-234) is a multitarget, potent, and CNS permeable inhibitor with IC50 of 5.2, 43, 350 and 460 nM for MAO-1, MAO-B, EeAChE and eqBuChE, respectively; inhibits Aβ aggregation, possesses antioxidant properties and protects from Aβ-induced apoptosis in vitro; completely blocks the aggregation mediated by AChE of both Aβ1-42 and Aβ1-40, showing a dual binding site to AChE; ASS234 significantly reduces Aβ1-42-mediated toxicity in SH-SY5Y human neuroblastoma cells, ASS234 is a promising multitarget drug candidates with potential impact for Alzheimer's disease.
Octahydroaminoacridine succinate, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine succinate can be used for Alzheimer's disease (AD) research[1].
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain[1][2].
Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3][4].
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6].
MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.IC50 value: 10.07 (pKi)Target: nociceptin receptorMCOPPB trihydrochloride is a trihydrochloride form of MCOPPB that is a new nonpeptide nociceptin/orphanin FQ peptide (NOP)-receptor agonist with a pKi of 10.07 ± 0.01 for the human NOP receptor.
MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease[1].
β-Bag cell peptide is a neuroactive peptide. β-Bag cell peptide elevates cyclic AMP levels in the bag cell neurons. β-Bag cell peptide decreases the amplitudes of the voltage-dependent potassium currents[1].
L-Alanine-1-13C,15N (L-2-Aminopropionic acid-1-13C,15N) is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Isomaltopaeoniflorin is a metabolite of the Chinese herbal formula Shuyu. Shuyu is a depression-like disease inhibitor[1].
MAO-B-IN-23 (Compound 11f) is a reversible and competitive MAO-B inhibitor (IC50: 1.44 μM, Ki: 0.51 μM)[1].
Piracetam-d8 (UCB-6215-d8) is the deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders[1][2].
(D-Asp1)-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[1].
6-Alpha Naloxol(Alpha-Naloxol) is an opioid antagonist closely related to naloxone; a human metabolite of naloxone.IC50 value:Target: opioid antagonistWhen responding over the entire 30 min operant session was examined, naloxone was only 5-fold more potent than 6-alpha-naloxol in suppressing operant responding under Morphine Na ve conditions, but this increased to a 65-fold potency difference after Single or Repeat Morphine pretreatment. Examination of the relative potency of these antagonists in the Early Phase of operant testing (5-15 min post-antagonist) revealed an even greater 100-fold potency difference between naloxone and 6-alpha-naloxol, but in the Late Phase of testing (25-35 min post-antagonist), this had declined to a 9-fold potency difference, comparable to the relative potency of naloxone to 6-alpha-naloxol under Morphine-Na ve conditions.
MPPG is a potent and selective L-AP4-sensitive receptor antagonist with an kD value of 9.2 μM, being tested on the neonatal rat spinal cord[1].
Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.