(R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
Fasciculin-II (Fas-2) is a potential inhibitor of acetylcholinesterase (AChE)[1].
Elinzanetant is a neurokinin receptors antagonist used for the research of Schizophrenia[1].
MDA 19 is a selective human CB2 receptor agonist with Ki of 43.3 nM. IC50 Value: 43.3 nM(Ki)Target: CB2 receptorin vitro: MDA19 displayed 4-fold-higher affinity at the human CB(2) than at the human CB1 receptor (K(i) = 43.3 +/- 10.3 vs 162.4 +/- 7.6 nM) and nearly 70-fold-higher affinity at the rat CB2 than at the rat CB1 receptor (K(i) = 16.3 +/- 2.1 vs 1130 +/- 574 nM). In guanosine triphosphate (GTP)gamma[(35)S] functional assays, MDA19 behaved as an agonist at the human CB1 and CB2 receptors and at the rat CB1 receptor but as an inverse agonist at the rat CB2 receptor. In 3',5'-cyclic adenosine monophosphate (cAMP) assays, MDA19 behaved as an agonist at the rat CB1 receptor and exhibited no functional activity at the rat CB(2) receptor. In extracellular signal-regulated kinases 1 and 2 activation assays, in vivo: MDA19 behaved as an agonist at the rat CB2 receptor. MDA19 attenuated tactile allodynia produced by spinal nerve ligation or paclitaxel in a dose-related manner in rats and CB2(+/+) mice but not in CB2(-/-) mice, indicating that CB2 receptors mediated the effects of MDA19. MDA19 did not affect rat locomotor activity.
β2AR agonist /M-receptor antagonist-1 is a potent dual muscarinic antagonist/beta 2 agonist (MABA). β2AR agonist /M-receptor antagonist-1 potently relaxes either Carbachol (HY-B1208)-induced contraction, in the absence (MABA) or presence of Propranolol (M3; HY-B1208), or Histamine (HY-B1204)-induced contraction (β2)[1][2].
Nimbin is a intermediate limonoid isolated from Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin can across blood-brain barrier[1][2][3].
Lanicemine (AZD6765) dihydrochloride is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects[1].
Neuromedin B (NMB) is a member of Bombesin (BN)-like peptide family in mammals.
Celaphanol A is a diterpene that can be isolated from the root bark of Celastrus orbiculatus. Celaphanol A shows neuroprotective effect against a hydrogen peroxide-induced cytotoxicity in PC12 cells[1].
Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
Ciproxifan(FUB-359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: 9.2 nM(Ki)Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
Tiagabine(NO328) is a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.Target: GABA reuptake inhibitorTiagabine had an early onset of effect, as shown by significant reduction from baseline in mean HAM-A total score compared with placebo at week 1 (observed cases, p < .05). Tiagabine was generally well tolerated and not associated with changes in sexual functioning or depressive status. Symptoms of a discontinuation syndrome during taper were not observed. Tiagabine may be a useful treatment option for adult patients diagnosed with GAD [1]. Tiagabine was generally well tolerated; the most common adverse events were nausea, dizziness and headaches [2]. Tiagabine (0.1 microM), an antiepileptic drug that specifically inhibits the GAT-1 GABA transporter inhibited GABA uptake 50% in temporal cortex and 60-68% in white structures [3].
6-Iodopravadoline (AM630) is a selective CB2 antagonist with Ki of 31.2 nM, and displays 165-fold selectivity over CB1 receptors.
AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia[1].
Acetyl-ACTH (7-24) (human, bovine, rat) causes a marked decrease of ACTH-evoked corticosterone and aldosterone release[1].
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol. IC50 Value:Target: β2-adrenergic receptorLevosalbutamol and salbutamol produced significantly better bronchodilator responses than placebo. Both the drugs showed equivalent time-dependent bronchodilator responses as measured by area under curve for percent change in FEV(1) and FVC over 6h. The time to onset of action, mean maximum bronchodilator response and duration of bronchodilator response were similar between levosalbutamol and salbutamol [1].
ADR 851 is a dopamine D2 receptor antagonist,and can be used in research on antiemetics[1].
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].
QX-314 chloride is a membrane-impermeable permanently charged sodium channel blocker[1].
Neamine tetrahydrochloride, a degradation product of Neomycin, is a broad-spectrum aminoglycoside antibiotic. Neamine tetrahydrochloride is an anti-angiogenesis agent targeting angiogenin. Neamine tetrahydrochloride has potent antibacterial, antitumor and neuroprotective activities[1][2].
Aβ-IN-4 (compound 12) is a potent amyloid β (Aβ) inhibitor. Aβ-IN-4 inhibits Aβ42 aggregation. However, Aβ-IN-4 can not alleviate the neurotoxicity of Aβ42 in SH-SY5Y cells. Aβ-IN-4 can not change the aggregation state of Aβ42 into a nontoxic one[1].
RL648_81 is a specific KQT-like subfamily 2/3 (KCNQ2/3) activator with an EC50 of 190 nM. RL648_81 robustly shifts the V1/2 of KCNQ2/3 channels towards hyperpolarized potentials.RL648_81 does not shift the V1/2 of either KCNQ4 or KCNQ5.RL648_81 has the potential for neurologic disorders associated with neuronal hyperexcitability research[1].
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia[1]。
β Amyloid(28-35) human is a β-amyloid peptide (Abeta), a lipid-induced amyloid core fragment. β Amyloid oligomers are neurotoxic, and β Amyloid(28-35) human can interact with neuronal membranes, regulate secondary structure and neurotoxicity, and cause Alzheimer's disease. β Amyloid(28-35) human has anisotropic effects on the acidic phospholipid DPH, resulting in enhanced internal fluidity of lipid membrane bilayers[1].
MAO-B-IN-15 is a selective MAO-B inhibitor (IC50: 13.5 μM) that forms π-π interaction with Tyr 326 residue. MAO-B-IN-15 can be used in the research of Parkinson’s disease[1].
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM[1][2][3].
Quinoprazine is a potent inhibitor of Vaccinia virus DNA synthesis with an IC50 value of 10 μM. Quinoprazine has antimalarial activity against Plasmodium berghei and also displays antiprion potency, significantly decreases PrPSc levels[1]-[5].
BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses[1].
RIPK1-IN-15 (Compound 2.5) is a potent inhibitor of RIPK1. RIPK1-IN-15 has the potential for the research neurodegenerative, autoimmune, and inflammatory diseases[1].