2. Neurological Disease

Neurological Disease

Neurological Disease

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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, stroke‐like episodes and dementia and depend on the part of the nervous system affected.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-115500
    PL265 1206514-50-2 98%
    PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4). PL265 can be used in non-addictive chronic pain research.
    PL265
  • HY-115511
    PyP-1 1370527-16-4 98%
    PyP-1 is a highly selective and potent PDE10 inhibitor. PyP-1 has a strong inhibitory effect on human PDE10A2 enzyme (Ki = 0.32 nM). PyP-1 can improve cognitive behavior. PyP-1 commonly used in research on conditions such as schizophrenia and cognitive impairment.
    PyP-1
  • HY-115596
    BTT-369 2413939-96-3 98%
    BTT-369 is a CaVα1·CaVβ3 protein-protein complex antagonist with a Ki of 2.0 μM. BTT-369 inhibits CaV2.2 currents, with an apparent IC50 value of 31 μM. BTT-369 disrupts the interaction between CaVα1 and CaVβ3 subunits. BTT-369 reduces the current density of CaV2.2, and shifts the voltage dependence of steady-state inactivation and activation of CaV2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain.
    BTT-369
  • HY-115606
    ML077 1135304-61-8 98%
    ML007 is a selective antagonist targeting the neuron-specific potassium-chloride co-transporter 2 (KCC2) with an IC50 for KCC2 is 537 nM, while its inhibitory activity on KCC1 is extremely weak (IC50 > 50 μM). ML077 inhibits the chloride ion excretion function of KCC2, increasing the intracellular chloride ion concentration, thereby enhancing the depolarization mediated by chloride ion channels. ML007 can promote glucose-stimulated insulin secretion (GSIS) without relying on KATP channels. ML007 can be used to study the functions related to pain, epilepsy, and insulin secretion.
    ML077
  • HY-115706
    13-Dilignoceroyl glycerol 120639-92-1 98%
    13-Dilignoceroyl glycerol is a diacylglycerol containing lignoceric acid (HY-121883 ) at the sn-1 and sn-3 positions. Lignoceric 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.
    13-Dilignoceroyl glycerol
  • HY-115724
    FPPQ 1648745-46-3 98%
    FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.
    FPPQ
  • HY-115739
    RTIL 13 1009376-10-6 98%
    RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 μM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively.
    RTIL 13
  • HY-115750
    Nω-allyl-L-arginine 139461-37-3 98%
    Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O.
    Nω-allyl-L-arginine
  • HY-115763
    3-Aminopropylphosphinic acid 103680-47-3 98%
    3-Aminopropylphosphinic acid (3-APPA) is a phosphonic analog of GABA. 3-Aminopropylphosphinic acid is a potent, selective GABAB receptor agonist.
    3-Aminopropylphosphinic acid
  • HY-115764
    nAChR agonist 2 252870-46-5 98%
    nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM).
    nAChR agonist 2
  • HY-115765
    N6-Benzyl-5'-ethylcarboxamido adenosine 152918-32-6 98%
    N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.
    N6-Benzyl-5'-ethylcarboxamido adenosine
  • HY-115782
    VU6001192 1821325-29-4 98%
    VU6001192 is a potent and selective mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator. VU6001192 has potent inhibitory activity against the mGlu2 receptor (IC50 = 207 nM), but no activity against the mGlu3 receptor and the other 6 mGlu subtypes. VU6001192 can be used for the research of neurological disease, such as depression.
    VU6001192
  • HY-115806
    TC9-305 2092914-16-2 98%
    TC9-305 is a potent and selective apoptosis inhibitor. TC9-305 has strong inhibitory activity against both Bim and tBid-induced apoptosis with EC50 values of 0.42 and 0.23 μM. TC9-305 can maintain the mitochondrial membrane potential, reduce ROS production, prevent the release of cytochrome c and block the upstream pathways of mitochondrial-mediated apoptosis. TC9-305 can be used for the research of neurological disease, such as storke.
    TC9-305
  • HY-115844
    LY-99335 78738-97-3 98%
    LY-99335 is an anesthetic antagonist with behavioral inhibitory activity. LY-99335 exhibits large dose separation at specific doses, indicating its potential in anesthetic antagonism.
    LY-99335
  • HY-115851
    Demethyl PL265 1206514-62-6 98%
    Demethyl PL265 is an enduring dual ENKephalinase inhibitor (DENKi) that holds promise for pain relief.
    Demethyl PL265
  • HY-115854
    Ro 15-1310 78756-33-9 98%
    Ro 15-1310 is an imidazobenzodiazepine that exhibits high affinity and selectivity for alpha 5-containing GABAA receptors. Ro 15-1310 is promising for research of convulsions.
    Ro 15-1310
  • HY-115856
    Sch 50910 790633-59-9 98%
    Sch 50910 is a GABA(B) receptor antagonist with some activity in inhibiting GABA(B) autoreceptors. Sch 50910 had no effect on electrically stimulated release at a concentration of 100 μM. The activity of Sch 50910 suggests that it may not have a significant role in studies of GABA(B) receptor function.
    Sch 50910
  • HY-115857
    SH-053-S-CH3-2'F 872874-00-5 98%
    SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs.
    SH-053-S-CH3-2'F
  • HY-115860
    TAS-4 794544-99-3 98%
    TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects.
    TAS-4
  • HY-115861
    UCM765 944284-77-9 98%
    UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies.
    UCM765
Cat. No. Product Name / Synonyms Application Reactivity