Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence[1][2].
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways[1][2].
Chloroprocaine hydrochloride (2-Chloroprocaine hydrochloride) is a potent inhibitor of Na,K-ATPase activity with an IC50 of 13 mM. Chloroprocaine hydrochloride blocks peripheral nerve[1].
N-[(1R)-4-[(Aminoiminomethyl)amino]-1-[[[(1R)-1-(4-hydroxyphenyl)ethyl]amino]carbonyl]butyl]-α-phenylbenzeneacetamide is an anticonvulsant agent with potential for the treatment of generalized tonic-clonic and partial seizures.
BMS-193885 (L-Lactic acid) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. BMS-193885 has a Ki value of 3.3 nM for the neuropeptide Y1 receptor, competitively acts on the neuropeptide Y binding site, and can reduce food intake and body weight through central Y1 inhibition[1].
Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
(±)-Equol is the racemate of equol. Equol is a metabolite of the soy isoflavones, daidzin and daidzein.
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo[1][2].
(Pro34)-Peptide YY (human) is a highly Y1-selective full agonist of Peptide YY (HY-P1514)/neuropeptide Y receptors[1].
Cl-NQTrp signifcantly disrupts the preformed fbrillar aggregates of Tau-derived PHF6 (VQIVYK) peptide and full-length tau protein[1][2].
Curcumenol is one of constituents in the plants of medicinally important genus of Curcuma[1].
Meclofenoxate hydrochloride, an ester of dimethylethanolamine (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown to improve memory, have a mentally stimulating effect, and improve general cognition.IC50 value: Target: nootropicMeclofenoxate, administered in a dose of 50 mg/kg twice daily for 7 days using the maze-training method, increased the number of responses to the conditioned stimulus, when retention tests were made 24 hours and 7 days after training, whereas citicholine, applied in the same way in a dose of 10 mg/kg, shortened the latency of the responses with reinforcement during the training and increased the number of correct responses to the conditioned stimulus in retention tests 7 days after the training [1]. Meclofenoxate appears to increase the consolidation of new information into long-term memory, but does not affect other aspects of remembering [2].
(E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington’s disease[1].
Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
Novel upregulator of TRIB1 expression, leading to reprogramming of hepatic lipoprotein metabolism from lipogenesis to scavenging
Triflupromazine hydrochloride is an antipsychotic medication, which are Dopamine D1/D2 receptor antagonists.
Galanin Receptor Ligand M35 is a high-affinity galanin receptor ligand acting as a galanin receptor antagonist in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human GalR1 and GalR2, respectively[1][2].
SMND-309 is a novel derivative of salvianolic acid B, and has shown protective effects against rat cortical neuron damage in vitro and in vivo. IC50 value:Target: SMND-309 mitigated the effects of ischemia and reperfusion injury on brain by decreasing the infract volume, improving neurological function, increasing the survival of neurons and promoting angiogenesis by increasing the levels of erythropoietin (EPO), erythropoietin receptor (EPOR), phosphorylated JAK2 (P-JAK2), phosphorylated STAT3 (P-STAT3), VEGF and VEGF receptor 2 (Flk-1) in the brain.
(RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors[1][2].
CP-809101 Hcl is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively. IC50 Value: 9.96(pEC50 for 5-HT2C); 7.19(pEC50 for 5-HT2B); 6.81(pEC50 for 5-HT2A)Target: 5-HT2C ReceptorCP-809101 is a potent, functionally selective 5-HT2C agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to assess the efficacy of a selective 5-HT2C agonist in animal models predictive of antipsychotic-like efficacy and side-effect liability. Similar to currently available antipsychotic drugs, CP-809101 dose-dependently inhibited conditioned avoidance responding (CAR, ED50 = 4.8 mg/kg, sc). CP-809101 antagonized both PCP- and d-amphetamine-induced hyperactivity with ED50 values of 2.4 and 2.9 mg/kg (sc), respectively and also reversed an apomorphine induced-deficit in prepulse inhibition. At doses up to 56 mg/kg, CP-809101 did not produce catalepsy. Thus, the present results demonstrate that the 5-HT2C agonist, CP-809101, has a pharmacological profile similar to that of the atypical antipsychotics with low extrapyramidal symptom liability. CP-809101 was inactive in two animal models of antidepressant-like activity, the forced swim test and learned helplessness.
DynaMin inhibitory peptide, myristoylated is a DynaMin inhibitor to interfere with the binding of amphiphysin with dynamin. DynaMin inhibitory peptide, myristoylated is a membrane-permeant form of the peptide that prevents endocytosis[1].
Diperodon is a local anaesthetics, by the action of hydrolazes in blood serum is decomposed.
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid[1]. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[2][3].
Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters.
Rivanicline (RJR-2403) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).IC50 value: 26 nM [1]Target: α4β2 nAChRin vitro: At concentrations up to 1 mM, Rivanicline does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that Rivanicline is less than one-tenth as potent as nicotine with greatly reduced efficacy. Rivanicline does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 > 1 mM). Chronic exposure of M10 cells to Rivanicline (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1].in vivo: Rivanicline significantly improved passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats with ibotenic acid lesions of the forebrain cholinergic projection system in an 8-arm radial maze paradigm. By comparison, Rivanicline was 15 to 30-fold less potent than nicotine in decreasing body temperature, respiration, Y-maze rears and crosses and acoustic startle response [2]. Metanicotine was about 5-fold less potent than nicotine in the tail-flick test after s.c administration, but slightly more potent after central administration [3].
LY288513, a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 possesses both anxiolytic and antipsychotic potential[1][2][3].