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mAChR modulator
Rapacuronium bromide is an allosteric modulator of muscarinic acetylcholine receptor (mAChR). -
chemoprotective agent
Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation. -
gamma secretase inhibitor
BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. -
NMDA receptor antagonist
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor. -
NMDA NR2B antagonist
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions. -
nAChR agnoist
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits. -
P2X7 allosteric modulator
GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). -
P2Y12 receptor inhibitor
Clopidogrel is a well-known and orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. -
nAChR agonist
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2 nAChRs (Ki=16 nM) and shows high selectivity for α6β2 and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [3H] cytisine sites is 16.7 nM.
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GABAAα5 modulator
Basmisanil is a highly selective GABAAα5 negative allosteric modulator. -
Aβ-ABAD inhibitor
Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.
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BACE-1 inhibitor
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. -
GABAA receptor partial agonist
CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity. -
mAChR antagonist
mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM. -
cholinesterase inhibitor
(R)-Rivastigmine D6 (tartrate) is the deuterium labeled (R)-Rivastigmine, which is an cholinesterase inhibitor. - PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
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M3 muscarinic receptor antagonist
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. -
mAChR antagonist
mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM. -
mAChR5 modulator
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM. -
glucosylceramide synthase inhibitor
Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. -
α4β2 nAChR partial agonist
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. -
BACE1 inhibitor
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. -
partial benzodiazepine receptor agonist
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity. -
GABAA receptors agonist
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a selective agonist at GABAA receptors that contain α4-δ subunits, and has anxiolytic and sedative effects. -
Benzodiazepine inverse agonist
DMCM (hydrochloride) is Benzodiazepine inverse agonist that displays anxiogenic and potent convulsant activity. -
GlyT1 inhibitor
LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a. -
calmodulin inhibitor
Zaldaride maleate (CGS-9343B) is a potent and selective inhibitor of calmodulin. -
[3H](+)pentazocine binding inhibitor
Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM. -
P2Y12 receptor antagonist
Prasugrel (PCR 4099) Maleic acid is a platelet inhibitor with IC50 value of 1.8 μM. -
COX-2 inhibitor
Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood. -
NMDA receptor antagonist
7-Chlorokynurenic acid sodium salt is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). -
COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. -
NMDA receptor antagonist
SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7. -
NMDA receptor GluN2B antagonist
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC50 of 8.1 nM and 3.6 nM, respectively.
Neuronal Signaling
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