LY-368975 is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. LY-368975 reduces food consumption in rodents.
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage[1].
NBQX is a highly selective and competitive AMPA receptor antagonist.
CCG-203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
AGA-(C8R) HNG17, Humanin derivative is a potent humanin (HN) derivative. AGA-(C8R) HNG17, Humanin derivative completely suppresses neuronal cell death by Alzheimer's disease-relevant insults[1].
5-HT2C agonist-3 ((+)-19) is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 has antipsychotic drug-like activity. 5-HT2C agonist-3 blocks Amphetamine-induced hyperactivity[1].
M65 is a specific antagonist of PAC1 receptor that inhibits ANP secretion[1].
MAO-B-IN-2 is a selective and competitive inhibitor of MAO-B and BChE with IC50 values of 0.51 and 7.00 μM, respectively.
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist[1].
D-NAME (D-NG-nitroarginine methyl ester) hydrochloride is a potent nitric oxide synthase (NOS) inhibitor. D-NAME hydrochloride inhibits the activity of NOS, reducing the production of nitric oxide[1].
[D-Ala2]-Met-Enkephalinamide, an opioid peptide, is a potent opioid agonist. [D-Ala2]-Met-Enkephalinamide decreases bile flow by a central mechanism. [D-Ala2]-Met-Enkephalinamide has analgesic properties[1][2].
Timosaponin B III is a major bioactive steroidal saponin isolated from Anemarrhena asphodeloides Bge, and exhibits anti-inflammatory, anti-platelet aggregative and anti-depressive effects[1][2][3].
7-Chlorokynurenic acid is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM.
GSM-1 (GSM1) is a γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1, shows potent Aβ42-lowering effect (IC50=0.348 uM) in a cell-based assay; does not affect total Aβ and its C-terminal counterpart product, APP intracellular domain (AICD), selectively reduced the Aβ42 generation accompanied by an increase in Aβ38 in in-vitro assay; decreases the ratio of Aβ42 to Aβ40 to 60% in plasma and the ratio of Aβ42 to total Aβ to 65% in cerebrospinal fluid from baseline to postdosing in monkeys (30 mg/kg)
Desflurane is an airway irritant, acts as an anesthesia agent[1].
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119[1].
Dexmedetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.Target: Adrenergic alpha-2 ReceptorDexmedetomidine, acting at alpha(2A) adrenoceptors, must be present during the encoding process to decrease discrete cue fear memory; however, its ability to suppress contextual memory is likely the result of blocking the consolidation process [1]. Dexmedetomidine had no analgesic effects in alpha(2A)-adrenoceptor KO mice [2]. Dexmedetomidine was effective in blocking these sympathomimetic actions of cocaine even in all 7 subjects who were homozygous for the Del322-325 polymorphism in the alpha2C AR, a loss-of-function mutation that is highly enriched in blacks [3].
PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively[1]. Anti-hyperalgesic effect[1].
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception[1].
Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function[1][2][3][4].
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research[1].
α-Synuclein inhibitor 9 (Compound 20C) is an α-Synuclein inhibitor. α-Synuclein inhibitor 9 binds to cavities in mature α-synuclein fibrils and reduces the β-sheet structure. α-Synuclein inhibitor 9 inhibits A53T α-Syn aggregation. α-Synuclein inhibitor 9 has neuroprotective effect, improves brain functional connection and relieves motor dysfunction.α-Synuclein inhibitor 9 can be used for Parkinson’s disease (PD) research.[1].
Imipramine N-oxide is the metabolite of Imipramine. Imipramine is a tertiary amine tricyclic antidepressant[1][2].
Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites.
Neuropeptide Y (29-64), amide, human is a biologically active 36-amino acid peptide.
Aceglutamide is a psychostimulant and nootropic, used to improve memory and concentration.
FK962 is an enhancer of somatostatin release, exerts cognitive-enhancing actions[1].
α-Conotoxin AuIA is a potent and selective α3β4 n-nAChR inhibitor. α-Conotoxin AuIA is a α-conotoxin that can be isolated from Conus aulicus[1].
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects[1].