Brofaromine is a monoamine oxidase (MAO) inhibitor with IC50 of 0.2 μM for MAO-A.
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].
Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases[1]. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density[2].Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD[3].
Monoamine oxidase is an enzyme composed of different polypeptides. Monoamine oxidation catalyzes the oxidative deamination of various biological amines in brain and peripheral tissues by producing hydrogen peroxide. Monoamine oxidase plays an important role in maintaining the regulation of synaptic transmission, emotional behavior and other brain functions[1][2].
GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 also behaves as a noncompetitive CB1 antagonist. GW-405833 suppresses inflammatory and neuropathic pain[1][2].
(2R,3R)-Chlorpheg is a week antagonist of L-homocysteic acid (L-HCA) induced depolarization.(2R,3R)-Chlorpheg also is a weak N-methyl-D-aspartate (NMDA) antagonist[1].
Crenezumab (MABT 5102A; RG 7412) is a fully humanized anti-Aβ monoclonal antibody that binds multiple forms of Aβ, such as soluble, oligomeric and fibrillar, for use in Alzheimer's disease research[1].
tCFA15 is a trimethyl cyclohexenonic long chain fatty alcohol containing 15 carbon atoms on the side chain, promotes the differentiation of neurons, and may regulates Notch signaling.
Naloxone hydrochloride is a potent opioid receptor antagonist.
Icalcaprant is a kappa-opioid receptor antagonist[1].
Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM[1].
Uridine 5′-diphosphoglucose-13C6 (disodium) is the 13C labeled Uridine 5′-diphosphoglucose disodium salt[1]. Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR[2].
JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays[1].
Acetyl-Amyloid β-Protein (1-6) amide is a hexapeptide that contains a potential copper(II) binding site. Acetyl-Amyloid β-Protein (1-6) amide can be used for research of Alzheimer's disease and related disorders[1].
RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines.RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system[1].RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties[2].
Axillaridine A can be isolated from Sarcococca hookeriana var. digyna. Axillaridine A inhibits the catalytic activity of AChE[1].
Mas7, a structural analogue of mastoparan, is an activator of heterotrimeric Gi proteins and its downstream effectors.
PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively)[1]. PK-THPP increases breathing rate and induces respiratory alkalosis in rats[2].
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.Preparation of 2-[(4-benzyl)-1-piperidinyl)methyl]benzimidazole-5-ols as NMDA NR2B receptor antagonists for the treatment of neuropathic pain.By McCauley, James A.; Claremon, David A.; Liverton, Nigel J. From PCT Int. Appl. (2004), WO 2004048364 A1 20040610. NR2B-Selective N-Methyl-D-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted BenzimidazolesBy McCauley, John A.; Theberge, Cory R.; Romano, Joseph J.; Billings, Susan B.; Anderson, Kenneth D.; Claremon, David A.; Freidinger, Roger M.; Bednar, Rodney A.; Mosser, Scott D.; Gaul, Stanley L.; et alFrom Journal of Medicinal Chemistry (2004), 47(8), 2089-2096.
MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease[1][2][3].
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
RuBi-GABA is a new ruthenium-based caged GABA compound. RuBi-GABA photocleaves and releases GABA after being excited with visible wavelengths. RuBi-GABA produces gaba receptor-mediated currents[1].
Succinic acid tromethamine is a potent and orally active anxiolytic agent. Succinic acid tromethamine is an intermediate product of the tricarboxylic acid cycle. Succinic acid tromethamine can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[1][2][3].
3-(3-Hydroxyphenyl)-3-hydroxypropanoic acid is an endogenous metabolite present in Urine that can be used for the research of Autism[1][2].
A highly selective, potent, BBB penetrant and orally bioavailable 5-HT6R antagonist for the treatment of neurological disorders such as AD and schizophrenia; significantly restores both scopolamine- and MK-801-induced cognitive dysfunction and demonstrates antipsychotic potential. Alzheimer Disease Phase 2 Clinical
Otilonium Bromide is an antimuscarinic used as a spasmolytic agent.Target: mAChROtilonium bromide inhibited the generation of ACh-induced calcium signals in a dose dependent manner (IC50=880 nM) [1]. Otilonium, a clinically useful spasmolytic, behaves as a potent blocker of neuronal nicotinic acetylcholine receptors (AChR). Whole-cell Ba2+ currents (IBa) through Ca2+ channels of voltage-clamped chromaffin cells were blocked by otilonium with an IC50 of 6.4 microM. Otilonium inhibited the secretory responses induced by 10 s pulses of 50 microM DMPP with an IC50 of 7.4 nM [2]. Otilonium bromide may represent an effective treatment for irritable bowel syndrome because it reduces its predominant symptom (abdominal pain/ discomfort) more than placebo does [3]. ilonium bromide (OB) is a spasmolytic agent that blocks L-Type Calcium channels in human colonic smooth muscle. otilonium bromide is safe, well tolerated and superior to placebo in reducing the frequency of abdominal pain, severity of abdominal bloating and protecting from symptom relapse in IBS. These results further confirm that patients with IBS can improve during and following treatment with otilonium bromide [4].
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) inhibitor with Ki and EC50 of 1.54 nM and 3.61 nM, respectively[1]. Anti-tumor activities[2].
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex[1]. CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents[2].
Chromogranin A (324-337), human is a peptide fragment of chromogranin A, it can be isolated from human ileal carcinoid tumor. Chromogranin A is a soluble glycoprotein stored with hormones and neuropeptides in secretory granules of most (neuro)endocrine cells and neurons, and it is also a plasma marker of neuroendocrine tumors[1][2].
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease[1].