C3bot(154-182) is a C3 peptide enhances recovery from spinal cord injury by improving regenerative growth of descending fiber tracts. C3bot(154-182) represents a promising tool to foster axonal protection and/or repair, as well as functional recovery after traumatic CNS injury[1].
S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety[1].
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice[1].
Palmitoylglycine, a novel endogenous lipid, acts as a modulator of calcium influx and nitric oxide production in sensory neurons. Palmitoylglycine induces transient influx of calcium followed by nitric oxide production via calcium-sensitive nitric-oxide synthase enzymes. Palmitoylglycine potently inhibits heat-evoked firing of nociceptive neurons in rat dorsal horn[1].
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects[1][2].
KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1[1][2].
Benzonatate (Benzononatine) is a peripheral oral antitussive that dampens the activity of cough stretch receptors. Benzonatate has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite[1][2].
BB 0305179 (compound 59) is a potent anti-prion agent, with an IC50 of 4.7 μM. BB 0305179 inhibits the toxicity of a specific PrP mutant carrying a deletion in the hydrophobic domain [1].
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease[1].
TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).Target: RAGEin vitro: TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.[1]in vivo: The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2]
(Z)-KC02 is an inhibitor of ABHD16A, the phosphatidylserine (PS) lipase that produces lyso-PS. Lysophosphatidylserine (lyso-PS) is a signaling lipid that regulates immune and neurological processes. It is associated with several neurological disorders such as retinitis pigmentosa and cataracts (PHARC). (Z)-KC02 depletes lyso-PS in lymphoblasts from PHARC subjects. (Z)-KC02 also reduces lyso-PS and lipopolysaccharide-induced cytokine production in macrophages and modulates lyso-PS metabolism in vivo[1].
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions[1][2].
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Clidinium bromide is an anticholinergic (specifically a muscarinic antagonist) drug, may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines.
D-Serine-d3 ((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration[1][2][3].
Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Macrozamin is a major constituent principle of Cycads. Macrozamin has carcinogenic, mutagenic, teratogenic and neurotoxic properties[1].
2-(Phosphonooxy)benzoic acid is a non-acetylated salicylic acid derivative which is used for treating inflammatory disease as well as in analgesic therapy[1].
Emapunil(AC-5216;XBD-173) is a translocator protein[TSPO (18 kDa)] ligand.IC50 value:Target: TSPO ligandXBD173 enhanced gamma-aminobutyric acid-mediated neurotransmission and counteracted induced panic attacks in rodents in the absence of sedation and tolerance development. XBD173 also exerted antipanic activity in humans and, in contrast to benzodiazepines, did not cause sedation or withdrawal symptoms [1]. The selective TSPO ligand, XBD173 (AC-5216, Emapunil), exerts anxiolytic effects not only in animal models, but also in human volunteers [2].
FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.
S-MTC is a selective type I nitric oxide synthase (NOS) inhibitor.
Biotin-β-Amyloid (1-40) is a N-terminal-labelled biotinylated amyloid-ß-(1-40) peptide.
Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin. IC50 Value: Target: SSRIsPipofezine is a tricyclic antidepressant (TCA) approved in Russia for the treatment of depression. In addition to its antidepressant action, pipofezine has sedative effects as well, indicating antihistamine activity.
5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a Ki of 1.43 nM.
M1/M2/M4 muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 3.2 nM, 32 nM and 1.7 nM, respectively[1].
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].
ω-Conotoxin MVIIC is a N- and P/Q-type Ca2+ channel blocker, significantly suppresses the 11-keto-βboswellic acid-mediated inhibition of glutamate release[1].
Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM)[1].
Acesulfame potassium is an artificial sweetener. Acesulfame potassium (long-term) affects cognitive functions, potentially via altering neuro-metabolic functions in mice[1].
Kadsurenin B is a PAF (platelet-activating factor) antagonist with neuroprotective activity. Kadsurenin B has a wide range of pharmacological research potential, such as antibacterial, anti-inflammatory, neuroprotective, antioxidant, antiplatelet aggregation, cytotoxic, antiparasitic, etc[1][2].