Azemiopsin is a potent nicotinic acetylcholine receptor (nAChR) inhibitor with IC50s of 0.18 μM and 22 μM against T. californica nAChR and human α7 nAChR, respectively. Azemiopsin blocks acetylcholine-induced currents in Xenopus oocytes heterologously expressing human muscle-type nAChR[1].
Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine[1].
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].
[Leu5]-Enkephalin is a pentapeptides with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.
Aromadendrane-4β,10α-diol is a sesquiterpene alcohol. Aromadendrane-4β,10α-diol significantly ameliorates the Aβ1-42 peptide-induced memory impairment. Aromadendrane-4β,10α-diol can be used for Alzheimer's disease (AD) research[1].
PKM2-IN-3 is a inhibitor of PKM2 kinase with IC50 value of 4.1μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation[1].
L-689560 is a potent N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. L-689560 is widely used as a radiolabeled ligand in binding studies and used for study the roles of NMDA receptors in normal neurological processes as well as in diseases[1][2].
Flavoxate-d4 hydrochloride (Rec-7-0040-d4) is the deuterium labeled Flavoxate hydrochloride. Flavoxate Hydrochloride is a muscarinic AChR antagonist used in various urinary syndromes and as an antispasmodic[1][2].
Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities[1][2][3].
Remternetug is a humanized immunoglobulin G1-kappa, anti-APP (amyloid beta A4 precursor protein) Aβ42 N3pGlu peptide monoclonal antibody. Remternetug recognizes a pyroglutamated form of Aβ that aggregates into amyloid plaques[1].
Picfeltarraenin X, a triterpenoid isolated from Picria fel-terrae Lour, is an AChE inhibitor[1].
Raclopride-d5 (hydrochloride) is the deuterium labeled Raclopride. Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively[1][2].
Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0%[1].
Grayanotoxin II is a potent analgesic agent, is a diterpenoid. Grayanotoxin II shows significant analgesic activity[1].
PACAP (1-38), human, ovine, rat is a neuropeptide with 38 amino acid residues. PACAP (1-38) binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively.
Mrgx2 antagonist-2 is a Mrgx2 antagonist (Example 123 in reference patent) with a pIC50 of 8.6. Mrgx2 antagonist-2 can be used in the research of MrgX2 -mediated diseases or disorders[1].
RU 23686 free base is a piperidinylindole derivative. RU 23686 free base can be used to investigate the extent to which different neurotransmitters by the interaction with pharmacological agents[1].
Eletriptan-d3 (Eletriptan-d3 HBr) is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
XJB-5-131 is a mitochondria-targeted ROS and electron scavenger[1]. XJB-5-131 is a bi-functional antioxidant that comprises a radical scavenger. XJB-5-131 is a synthetic antioxidant that targets mitochondria[2]. XJB-5-131 is an effective ionizing irradiation protector and mitigator of cord blood mononuclear cells (CB MNCs)[3].
Desmethylnortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1].
Hydroquinidine is an antiarrhythmic agent.
A new tertiary amine, Oxyphencyclimine hydrochloride，has been investigated for its effects on the peripheral parasympathetic system. was essentially the most potent in depressing gastric secretion.
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment[1][2].
PF-00217830 is a serotonin 1A receptor agonist, dopamine D2 receptor agonist, and serotonin 2A receptor antagonist.PF-00217830 may be used in the study of schizophrenia.
IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].
Tetrabenazine is a VMAT-inhibitor used for treatment of hyperkinetic movement disorder.Target: Otherstetrabenazine (TBZ), a monoamine-depleting and a dopamine-receptor-blocking drug. TBZ is an effective and safe drug for the treatment of a variety of hyperkinetic movement disorders. In contrast to typical neuroleptics, TBZ has not been demonstrated to cause tardive dyskinesia [1, 2]. Twenty patients with tardive dyskinesia (mean duration = 43.7 months) were videotaped before and after tetrabenazine treatment. One patient did not tolerate tetrabenazine owing to sedation. The remaining 19 were rated after a mean of 20.3 weeks at a mean tetrabenazine dose of 57.9 mg/day. There were significant improvements in mean scores on both the patient AIMS self-rating and the AIMS motor subset evaluated by the blind videotape raters. All 19 patients continued to take tetrabenazine after the study [3].
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth[1][2][3][4].
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively[1].
Thiorphan is a selective NEP (neprilysin) inhibitor with an IC50 of 6.9 nM[1].