DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.Target:PBRin vitro: DAA1106 binding to PBR was significantly increased in widespread areas in MCI subjects when compared to healthy controls.[1] DAA-1106 is a drug which acts as a potent and selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO, but with no affinity at the GABAA receptor. [2]in vivo: DAA-1106 has anxiolytic effects in animal studies. DAA-1106 has a sub-nanomolar binding affinity (Ki) of 0.28nM, and has been used extensively in its 3H or 11C radiolabelled form to map TSPO in the body and brain, which has proved especially helpful in monitoring the progress of neurodegenerative diseases such as Alzheimer's disease. [2]
UK-240455 is a potent and selective N-methyl D-aspartate (NMDA) glycine site antagonist.
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A)[1].
DHBP dibromide is an inhibitor for calcium release and a muscle relaxant.
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].
Istaroxime hydrochloride is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM.
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].
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research[1].
ONT-093 is a potent inhibitor of P-glycoprotein pump. ONT-093 has the potential for the research cancer diseases[1].
Aminooxyacetic acid (Carboxymethoxylamine) is a malate-aspartate shuttle (MAS) inhibitor. Aminooxyacetic acid also inhibits the GABA degradating enzyme GABA-T.
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].
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].
AMPA receptor antagonist-2 (example 23) is an AMPA receptor antagonist[1].
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate hydrate (2:1:4) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM[1][2].
Omeprazole magnesium is an orally active proton pump inhibitor (PPI) and can suppress gastric acid. Omeprazole magnesium can be used for acid reflux-related symptoms and frequent heartburn research[1][2].
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a hERG channel blocker with an IC50 of 0.23 μM[1]. Aprindine hydrochloride has inhibitory effects on Na+/Ca2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias treatment research[2].
CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand[1]. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7[2].
(S)-(-)-Levamisole (Levamisole), an anthelmintic agent with immunomodulatory properties. (S)-(-)-Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active[1][2].
Pregnanolone sulfate pyridinium is an endogenous neurosteroid that inhibits NMDA receptors and is neuroprotective[1].
Isonipecotic acid is a GABAA receptor partial agonist[1].
McN5691 is a voltage-sensitive calcium channel blocker.
UK-52831, a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.
MSP-3 is a potent TRPV1 agonist, with an EC50 of 0.87 μM. MSP-3 exhibits neuroprotective and antinociceptive effects[1].
Nav1.7-IN-6 (example 346) is a Nav1.7 selective inhibitor, which is extracted from patent WO2015078374A1[1].
HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2[1].
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].