Neurological Disease A range of neurological disorders, including epilepsy and dystonia, may involve dysfunctional intracortical inhibition, and may respond to treatments that modify it. Parkinson’s is a neurodegenerative disease characterized by increased activity of GABA in basal ganglia and the loss of dopamine in nigrostriatum, associated with rigidity, resting tremor, gait with accelerating steps, and fixed inexpressive face. Neurological deficits, along with neuromuscular involvement, are characteristic of mitochondrial disease, and these symptoms can have a dramatic impact on patient quality of life. Neurological features may be manifold, ranging from neural deafness, ataxia, peripheral neuropathy, migraine, seizures, strokelike episodes and dementia and depend on the part of the nervous system affected. www.MedChemExpress.com 1 Neurological Disease Inhibitors & Modulators (+)-Cevimeline hydrochloride hemihydrate (+)-Dihydrexidine hydrochloride Cat. No.: HY-76772A (DAR-0100 hydrochloride) Cat. No.: HY-101299 Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: (+)-Dihydrexidine hydrochloride is a dopamine D1 receptor receptor agonist, is a candidate therapeutic drug for agonist with an EC50 of 72± 21 nM. xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR The general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 1 mg, 5 mg (+)-MK 801 Maleate (+)-PD 128907 hydrochloride (Dizocilpine maleate; Dizocilpine hydrogen maleate) Cat. No.: HY-15084 Cat. No.: HY-110000 Bioactivity: (+)-MK 801 Maleate is a potent, selective and non-competitive Bioactivity: (+)-PD 128907 hydrochloride is a selective dopamine D2/D3 NMDA receptor antagonist with Kd of 37.2 nM in rat brain receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D membranes. 3 receptors, 179, 770 n M for human and rat D 3 receptors, respectively. Purity: 99.98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg (+)-PHENSERINE (-)-(S)-Equol Cat. No.: HY-16009 Cat. No.: HY-100583 Bioactivity: Posiphen is a novel selective cholinesterase noncompetitive Bioactivity: (-)-(S)-Equol is a high affinity ligand for estrogen receptor inhibitor with an IC50 of 45.3 μM. β with a Ki of 0.73 nM. Purity: >98% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg (-)-Aspartic acid (-)-Borneol ((R)-Aspartic acid; D-(-)-Aspartic acid) Cat. No.: HY-42068 (L-Borneol) Cat. No.: HY-N1368B Bioactivity: (-)-Aspartic acid is an endogenous NMDA receptor agonist. Bioactivity: (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM. Purity: 97.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g 100 mg (-)-Cevimeline hydrochloride hemihydrate (-)-Huperzine A Cat. No.: HY-76772B (Huperzine A) Cat. No.: HY-17387 Bioactivity: Cevimeline hydrochloride hemihydrate, a novel muscarinic Bioactivity: Huperzine A, an active Lycopodium alkaloid extracted from receptor agonist, is a candidate therapeutic drug for traditional Chinese herb, is a potent, selective and xerostomia in Sjogren's syndrome. IC50 value: Target: mAChR reversible acetylcholinesterase (AChE) inhibitor and has been The general pharmacol. properties of this drug on the widely used in China for the treatment of Alzheimer's disease gastrointestinal, urinary, and reproductive systems and other… (AD). Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 5 mg, 10 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] (-)-MK 801 Maleate (-)-Securinine Cat. No.: HY-15084A Cat. No.: HY-N2079 Bioactivity: (-)-MK 801 Maleate is the enantiomer of (+)-MK-801. (+)-MK 801 Bioactivity: (-)-Securinine is plant-derived alkaloid and also a GABAA Maleate is a potent, selective and non-competitive NMDA receptor antagonist. receptor antagonist. Purity: 99.70% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg (1R,2R)-2-PCCA(hydrochloride) (1R,2S)-VU0155041 Cat. No.: HY-100013A1 Cat. No.: HY-14417A Bioactivity: (1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and Bioactivity: (1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial acts as a potent GPR88 receptor agonist, with an EC50 of 3 mGluR4 agonist with an EC50 of 2.35 μM. nM. Purity: 98.08% Purity: 98.42% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 5 mg, 10 mg, 25 mg (Arg)9 (R)-(-)-Rolipram (Nona-L-arginine; Peptide R9) Cat. No.: HY-P0133 ((R)-Rolipram; (-)-Rolipram) Cat. No.: HY-16900A Bioactivity: (Arg)9 (Nona-L-arginine;Peptide R9) is a cell-penetrating Bioactivity: (R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is peptide; exhibits neuroprotective activity with an IC50 of a selective inhibitor of phosphodiesterases PDE4 with IC50 of 0.78 μM in the glutamic acid model. Sequence: 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg. respectively. Purity: >98% Purity: 99.85% Clinical Data: Phase 2 Clinical Data: Phase 1 Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg (R)-5-Hydroxymethyl Tolterodine (R)-ADX-47273 (Desfesoterodine; PNU-200577) Cat. No.: HY-76569 Cat. No.: HY-13058B Bioactivity: (R)-5-Hydroxymethyl Tolterodine(PNU-200577; Desfesoterodine) Bioactivity: (R)-ADX-47273 is a potent mGluR5 positive allosteric is a potent and selective muscarinic receptor antagonist with modulator, with an EC50 of 168 nM for potentiation . a Kb and a pA2 of 0.84 nM and 9.14, respectively. Purity: 99.66% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg (R)-Baclofen (R)-Baclofen hydrochloride (STX209) Cat. No.: HY-17354 (STX 209 hydrochloride) Cat. No.: HY-17354A Bioactivity: (R)-Baclofen(STX209) is a selective GABAB receptor agonist. Bioactivity: (R)-Baclofen Hcl(STX-209 Hcl) is a derivative of IC50 value: Target: GABAB receptor GABAB receptors are gamma-aminobutyric acid (GABA) primarily used to treat metabotropic receptors which produce slow inhibitory signals. spasticity and is in the early research stages for use for the By manipulating GABAB receptor activity using Baclofen, a treatment of alcoholism. Target: GABA Baclofen (brand names variety of functions are studied including synaptic… Kemstro, Lioresal, Liofen, Gablofen, Beklo and Baclosan) is a… Purity: 98.0% Purity: >98% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in Water, Size: 10 mg, 50 mg 10 mg, 50 mg www.MedChemExpress.com 3 (R)-Oxiracetam (RS)-MCPG ((R)-(+)-Oxiracetam) Cat. No.: HY-17554 (alpha-MCPG) Cat. No.: HY-100371 Bioactivity: (R)-Oxiracetam is the (R)-enantiomer of the nootropic drug Bioactivity: (RS)-MCPG is a non-selective group I/group II metabotropic oxiracetam. Oxiracetam (ISF 2522) is a nootropic drug of the glutamate receptor antagonist. racetam family and stimulant. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg (S)-(-)-5-Fluorowillardiine (S)-(-)-5-Fluorowillardiine hydrochloride ((5S)-Fluorowillardiine; (S)-5-Fluorowillardiine) Cat. No.: HY-16713 ((5S)-Fluorowillardiine hydrochloride; …) Cat. No.: HY-16713A Bioactivity: (S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR Bioactivity: (S)-(-)-5-Fluorowillardiine Hcl is a potent and specific AMPAR agonist. agonist. Purity: >98% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg (S)-Glutamic acid (S)-MCPG ((+)-L-Glutamic acid) Cat. No.: HY-14608 ((+)-MCPG) Cat. No.: HY-100406 Bioactivity: (S)-Glutamic acid acts as an excitatory transmitter, shows a Bioactivity: (S)-MCPG is the active isomer of (RS)-MCPG (Cat. No. direct activating effect on the release of DA from HY-100371), non-selective group I/group II metabotropic dopaminergic terminals. glutamate receptor antagonist. In vivo: (S)-MCPG (20.8 μg) injected intraventricularly (i.c.v.) before testing impaired the performance of rats in the spatial version of the Morris… Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg, 50 mg (S)-Timolol Maleate (S)-Willardiine (Timolol Maleate) Cat. No.: HY-17380 ((-)-Willardiine) Cat. No.: HY-12499 Bioactivity: (S)-Timolol maleate, is a potent non-selective β-adrenergic Bioactivity: (S)-Willardiine is a potent agonist of AMPA/kainate receptors receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and with EC50 of 44.8 uM. IC50 value: 44.8 uM(EC50) [1] Target: β2 receptor subtypes respectively). IC50 Value: 1.97 nM(Ki for AMPA/kainate receptor agonist in vitro: The (S)- but not β1); 2.0 nM(Ki for β2) Target: β-adrenergic receptor (R)-isomers of willardiine and 5-bromowillardiine were potent (S)-Timolol, 50% bioavailability following oral… agonists, producing rapidly but incompletely desensitizing… Purity: 99.87% Purity: 98.70% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg 10 mg, 50 mg (Z)-Hexadec-9-enoic acid (Z)-Thiothixene Cat.