Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
Nizofenone is a neuroprotective agent which protects neurons from death following cerebral ischemia or anoxia. Nizofenone can be used in the research of acute neurological conditions, such as stroke[1][2][3].
(Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects[1][2].
(Rac)-Levomepromazine-d3 ((Rac)-Methotrimeprazine-d3) hydrochloride is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
D159687 is a selective PDE4D inhibitor[1].
Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor(SSRI).Target: SSRIDapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Premature ejaculation (PE) is the most common male sexual disorder, estimated to affect up to 30% of men. Dapoxetine is the only drug with regulatory approval for such an indication. The treatment of PE consists of primarily off-label use of oral selective serotonin reuptake inhibitors (SSRIs) via either on-demand or daily delivery.
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].
Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC50 values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.
Homatropine Bromide is muscarinic AChR antagonist that is an anticholinergic medication.Target: mAChRHomatropine is an anticholinergic medication that is an antagonist at muscarinic acetylcholine receptors and thus the parasympathetic nervous system. Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs [1]. Homatropine has similar affinities for muscarinic receptors in stomach (pA2 = 7.13) and for those in atria mediating force (pA2 = 7.21) and rate (pA2 = 7.07) responses [2]. Homatropine [14C]methylbromide administrated rectal achieves higher and rapid peak plasma concentrations than by the other routes in rats whether HMB-14C is administered in a water-soluble suppository base or in aqueous solution, retained 28% of the 14C has been excreted in the urine while 56% remained in the large intestine after 12 hours. Unlabelled Homatropine methylbromide, given in rectal suppositories to anaesthetized rats, causes prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure [3].
2-Propyl-2-pentenoic acid is a metabolite of Valproic acid (HY-10585). 2-Propyl-2-pentenoic acid has a facilitating action on the acquisition of conditioned behavior with negative reinforcement in mice[1].
Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain[1].
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models[1].
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is an opioid-receptor antagonist[1].
Melperone, a butyrophenone, is an antipsychotic drug used for sleep induction which is frequently prescribed in psychiatric setting[1]. Melperone has been used for a variety of indications, including the treatment of schizophrenia, but also for agitation in the elderly[2].
Corydaline is an acetylcholinesterase inhibitor isolated from Corydalis yanhusuo.
CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model[1].
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC50=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents [1].
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment [1]. Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex[2].
Lamotrigine-13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Tyrosylleucine (Tyr-Leu, YL) TFA, an orally active dipeptide, exhibits a potent antidepressant-like activity[1].
Dynorphin B (1-9) is a neuropeptide and N-terminal cleavage product of dynorphin B. The formation of dynorphin B (1-9) is blocked by N-ethylmaleimide (NEM), a non-selective inhibitor of cysteine peptidases[1].
P7C3-A20 is a derivative of P7C3 with potent neuroprotective activity.
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8)[1].
Smilagenin (SMI) is a lipid-soluble small-molecule steroidal sapogenin from Rhizoma anemarrhenae and Radix asparagi widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases[1]. Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density[2].Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD[3].
(2R,3R)-Chlorpheg is a week antagonist of L-homocysteic acid (L-HCA) induced depolarization.(2R,3R)-Chlorpheg also is a weak N-methyl-D-aspartate (NMDA) antagonist[1].
Crenezumab (MABT 5102A; RG 7412) is a fully humanized anti-Aβ monoclonal antibody that binds multiple forms of Aβ, such as soluble, oligomeric and fibrillar, for use in Alzheimer's disease research[1].
Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM[1].
Acetyl-Amyloid β-Protein (1-6) amide is a hexapeptide that contains a potential copper(II) binding site. Acetyl-Amyloid β-Protein (1-6) amide can be used for research of Alzheimer's disease and related disorders[1].
MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease[1][2][3].