NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research[1].
TAK-041 is a potent and selective GPR139 agonist with an EC50 of 22 nM. TAK-041 has the potential for the research of negative symptoms associated with schizophrenia[1].
MAO-B-IN-16 is a selective monoamine oxidase B (MAO-B) inhibitor, with an IC50 of 1.55 µM. MAO-B-IN-16 can be used in the study of central nervous disorders, such as parkinson's disease[1].
N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC50 of 21.3 μM[1].
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine[1].
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research[1].
Dynamin IN-1 is a potent dynamin inhibitor with an IC50 value of 1.0 µM[1].
Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
Lisuride (maleate) is a potent agonist of dopamine with a probably direct action on dopaminergic receptors. Lisuride (maleate) is an ergot derivative. Lisuride (maleate) releases the premenstrual mastalgia without significant side effects[1][2].
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 µM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups[1][2][3].
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor. Target: dopamine D2 receptor, prolactinQuinagolide is a selective, D2 receptor agonist (or prolactin-release inhibitor) that is used for the treatment of elevated levels of prolactin. Quinagolide is helpful in reducing prolactin levels to reduce milk production for certain medical reasons and to treat some types of infertility, breast problems and menstrual disorders. Quinagolide exerts a strong and specific inhibitory effect on prolactin release by acting directly on the prolactin-secreting cells of the anterior pituitary without reducing the levels of other pituitary hormones.
Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2].
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility[1][2].
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS)[1].
Hydroxydione has an effect of general anesthetic. Hydroxydione is a neuroactive steroid it can be used for anaesthesia related research[1][2].
LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease[1][2].
OMDM-3 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 16.6 μM[1].
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM[1].
Tideglusib is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3βWT (1 h preincubation) and GSK-3βC199A (1 h preincubation), respectively.
Biphenylindanone A (BINA) is a selective human mGluR2 (hmGluR2) potentiator for the treatment of many neurological disorders[1].
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect[1].
(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.Target: SSRIsFluvoxamine is effective in inhibiting 5-ht uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted [2]. Fluvoxamine was less potent at decreasing ethanol self-administration when food was available concurrently versus when ethanol was available in isolation [ED50: 4.0 (2.7-5.9) and 5.1 (4.3-6.0)]. Effects on food were similar under each condition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduled food reinforcement [3].Clinical indications: Depression; Obsessive compulsive disorder; Social phobia FDA Approved Date: December 5, 1994Toxicity: Anorexia, Constipation, Dry mouth, Headache, Nausea, Nervousness, Skin rash, Sleep problems, Somnolence, Liver toxicity, Mania, Increase urination, Seizures, Sweating increase, Tremors, or Tourette's syndrome.
L-Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine.Target: mAChRHyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care [1].
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research[1][2][3][4].
L 741742 hydrochloride is an orally active and selective antagonist of hD4 receptors. L 741742 hydrochloride has a good brain penetration. L 741742 hydrochloride can be used in study nervous system disorders, particularly schizophrenia[1].
LY-466195 is a competitive antagonist of GLUK5 receptor.
Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.