L-Glutamic acid-d5 is the deuterium labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC50 of 0.5 μM.
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].
Taltirelin acetate (TA-0910 acetate) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release)[1].
Galanin (1-13)-Neuropeptide Y (25-36) amide is a high-affinity ligand for galanin receptors, and galanin itself[1].
Phenylpiracetam(Phenotropyl; Phenotropil) is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam.IC50 Value:Target: AMPA receptor allosteric modulatorin vitro: N/Ain vivo: In the open-field test, a significant increase in locomotor activity was observed after a single administration of R-phenotropil at doses of 10 and 50 mg/kg and S-phenotropil at a dose of 50 mg/kg. In the forced swim test, R-phenotropil induced an antidepressant effect at doses of 100 and 50 mg/kg, and S-phenotropil was active at a dose of 100 mg/kg. R-phenotropil significantly enhanced memory function in a passive avoidance response test at a dose of 1 mg/kg; the S-enantiomer did not show any activity in this test [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].
(Rac)-SNC80 is a racemate of SNC80 (HY-101202). SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment[1][2][3][4][5][6].
Simufilam (PTI-125) dihydrochloride is a low toxicity, orally active filamin A (FLNA) activator. Simufilam dihydrochloride preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam dihydrochloride can be used for the research of Alzheimer's disease[1].
A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. IC50 value: Target: P2X2/3It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management.
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.
BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 can be used for the research of a mood disorder, post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorder[1].
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].
N-Methyl Duloxetine hydrochloride is an analgesic. N-Methyl Duloxetine (hydrochloride) elicits both tonic and use-dependent block of neuronal Na+ channels[1].
Hydroxy-2-[2-(2-hydroxyphenyl)ethyl]chromone is a neuroprotective agent[1]. Hydroxy-2-[2-(2-hydroxyphenyl)ethyl]chromone shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cell[1].
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.
Talsupram (hydrochloride) is a selective norepinephrine inhibitor with high affinity for norepinephrine transporter (NET) and can be used in the study of neuropathic pain[1].
Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed.
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].
NAV 26 (compound 26) is a selective voltage-gated sodium channel Nav1.7 blocker with an IC50 of 0.37 μM. NAV 26 can be used for pain research[1].
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].