Physostigmine hemisulfate (Eserine hemisulfate) is a potent cholinesterase inhibitor. Physostigmine hemisulfate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate induces reanimation from isoflurane anesthesia in adult rats[1].
Carphenazine is a phenothiazine antipsychotic agent. Carphenazine can be used for researching chronic schizophrenic psychoses[1].
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].
(±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist.
Opicapone is an available catechol-O-methyltransferase (COMT) inhibitor. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM.
FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic[1].
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia[1].
HL271, a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment[1][2].
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae[1][2].
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia[1][2].
TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2[1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter[1] [2].
Ralmitaront (RO6889450), a potent and orally active partial agonist of the trace amine-associated receptor 1 (TAAR1), acts as a neuroleptic agent. Ralmitaront can be used for the research of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder, and negative symptoms[1].
BCL6 ligand-1 (compound I-94) is a ligand for TCIP 1 (HY-156531). TCIP 1 is a BCL6 inhibitor that activates apoptosis and is used in cancer research[1].
ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD)[1].
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1].
αA-Conotoxin PIVA is a selective mouse musclenAChR inhibitor with IC50 for adult and fetal mouse musclenAChR sub> values are 2.3 nM and 22 nM respectively. αA-Conotoxin PIVA can be used in the study of neurological diseases.
(-)-Variabilin (compound 13) is an Neurogenin2 (Ngn2) promoter activator isolated from Butea superba. (-)-Variabilin promotes differentiation of neural stem cells into neurons[1].
(Thr4,Gly7)-Oxytocin, an Oxytocin analogue, is a specific OT receptor agonist. (Thr4,Gly7)-Oxytocin also excites subicular neurons via activation of TRPV1 channels, and depression of K+ channels. [1][2].
Ara-F-NAD+, an arabino analogue of NAD+, is a potent, slow-binding CD38 NADase inhibitor, with a Ki of 169 nM[1][2].
Alpertine is an antipsychotic agent extracted from patent US 5955459 A.
Astragaloside protects the morphological structures and restores acetylcholine level in rat hippocampus, and improves brain functions via normalizing brain EEG[1].
Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates[1]. Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms[2].
ITH12575, a CGP37157 derivative, is a potent and selective mNCX blocker. ITH12575 reduces Ca2+ influx through CALHM1 at low micromolar concentrations[1][2].
(1S,2R)-Tranylcypromine hydrochloride is a potent antidepressant agent. (1S,2R)-Tranylcypromine hydrochloride can inhibits MAO and LSD1[1][2].
Acetoxyvalerenic acid is a natural compound that could be found in valerian[1].
A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).IC50 Value: Target: P2X7in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1].