Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia[1][2].
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD)[1].
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat[1].
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease[1][2][3].
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research[1].
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].
N-Benzyloleamide is a maccamide isolated from Lepidium meyenii (Maca). N-Benzyloleamide irreversibly inhibits fatty acid amide hydrolase (FAAH). N-benzyloleamide influences the energy metabolism and reveals antioxidant and antifatigue activities[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.
LSP-GR3 is a novel chemically-modified RNA oligonucleotides, called splice modulating oligomers (SMOs), which potently and specifically modulate GluR alternative splicing to GluR3-flip expression throughout the CNS.
Velufenacin is a muscarinic receptor antagonist[1].
MLS1082 is a novel positive allosteric modulator of the D1 dopamine receptor, potentiatse dopamine-stimulated G-protein- and β-arrestin-mediated signaling and increase the affinity of dopamine for the D1 receptor with low micromolar potencies.
Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder[1][2].
Naratriptan-d3 is the deuterium labeled Naratriptan[1]. Naratriptan is a selective 5-HT1 receptor subtype agonist[2].
6-methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
BACE1-IN-2 is a 1,4-Oxazine β-Secretase 1 (BACE1) inhibitor with an IC50 of 22 nM[1].
3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) is a potent dopamine uptake inhibitor[1]. 3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) acts as a potent long-acting antihistaminic agent[2].
Imnopitant dihydrochloride is a neurokinin NK1 receptor antagonist[1].
Pirlindole is a novel potent inhibitor of Enteroviruse that targets Viral Protein 2C, inhibits EV-B and EV-D through the inhibition of genome replication (CV-B3 EC50=9.91 uM).
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors[1].
DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14)[1].
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.
UCM 608 is a high affinity melatonin (MT) membrane receptor agonist. The pKi values for MT1 and MT2 are 10.7 and 10.4[1][2].
MT-7716 free base (W-212393) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention[1].
[Nle11]-Substance P is a substance P analog that avoids methionine oxidation problems.
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.
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1][2].