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.
Aniracetam(Ro 13-5057) is a nootropics and neuroprotective drug, which is selectively modulates the AMPA receptor and nAChR.Target: AMPA; nAChRAniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam. It selectively modulates the AMPA receptor. It is lipid soluble and has possible cognition enhancing effects. It has been tested in animals extensively, Alzheimer's patients and temporarily-impaired healthy subjects. It has shown potential as an anxiolytic in three clinical animal models [1].Administration of aniracetam for 10 days (post-natal days (PND) 18-27), at a dose of 50 mg/kg reversed cognitive deficits in both rat genders, indicated by a significant increase in the number of avoidances and the number of 'good learners'. After the termination of the nootropic treatment, a significant increase in both amplitude and frequency of AMPA receptor-mediated mEPSCs in hippocampal CA-1 pyramidal cells was observed [2].Clinical indications: Cognitive disorder; StrokeFDA Approved Date: Toxicity: insomnia; headaches; nausea or rash.
Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC50 value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders[1][2].
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1)[1].
LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.
Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist[1][2].
CP-409092 is a GABA(A) partial agonist, used for the treatment of anxiety.
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation[1][2][3].
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats[1][2].
rel-Paroxetine hydrochloride is a isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. Cleavage at -Leu-Asp- of Mca-SEVNLDAEFK(Dnp) liberates the highly fluorescent 7-methoxycoumarin (Mca) fragment from the proximity quenching effect of the 2,4-dinitrophenyl (Dnp) internal quencher resulting in a large and easily detectable increase in fluorescence intensity.
GR 196429 is a melatonin receptor agonist with some selectivity for the MT1 subtype. GR-196429 produces both sleep-promoting effects and alterations of circadian rhythm, as well as stimulating melatonin release in mice.
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM[1]. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM[3].
YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr)[1].
Glycine-13C is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
FG8119 is a novel benzodiazepine agonist extracted from patent US 4745112 A.
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamine oxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress[1][2].
Fenoldopam-d4 (SKF-82526-d4) mesylate is the deuterium labeled Fenoldopam mesylate. Fenoldopam (SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist[1][2].
Vafidemstat is a dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
κ-Bungarotoxin (κ-Bgt) is a potent, selective, and slowly reversible antagonist of α3β2 neuronal nicotinic acetylcholine receptors with an IC50 of 2.30 nM[1].
Pitofenone hydrochloride, a spasmolytic compound, inhibits the acetylcholinesterase (AChE) activity from bovine erythrocytes and from electric eel with Kis of 36 and 45 μM, respectively.
Autophagy inducer D61 is a small molecule autophagy inducer with antibacterial activity, induces LC3II and promotes aggregation of LC3II near Salmonella.D61 (25 uM) reduced the bacterial load (GFP signal in RAW 264.7 macrophages) by 20-fold, with IC50 of 1.3 μM in the SAFIRE assay.D61 antibacterial activity depends on the VPS34 complex and on ATG5.D61 also reduced Salmonella load in the spleens and livers of infected mice.D61 antibacterial activity in macrophages is synergistic with the antibiotic chloramphenicol but that this synergy is largely independent of the known autophagy-stimulating activity of chloramphenicol.Salmonella enterica is a natural bacterial pathogen of humans and animals that causes systemic infection or gastroenteritis.
PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR)[1][2].PHA 568487 reduces neuroinflammation and oxidative stress[2]. PHA-568487 has rapid brain penetration[3].
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression[1].
Fluoxetine hydrochloride is an antidepressant and a selective serotonin reuptake inhibitor.
FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.
Droperidol is a Dopamine-2 Receptor Antagonist. Target: D2DRDroperidol is a butyrophenone, with anti-emetic, sedative and anti-anxiety properties.