S 17092 (S 17092-1) is a potent cerebral prolyl-endopeptidase (PEP) inhibitor with an IC50 of 1.2 nM. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging[1].
Protein Kinase C Peptide Substrate is targeted to a specific cellular compartment in a manner dependent on second messengers and on specific adapter proteins in response to extracellular signals that activate G-protein-coupled receptors, tyrosine kinase receptors, or tyrosine kinase-coupled receptors. Protein Kinase C Peptide Substrate then regulates various physiological functions including the activation of nervous, endocrine, exocrine, inflammatory, and immune systems[1].
NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide (41GCWMLY46 within the N-terminus of γD-crystallin) as well as full-length γD-crystallin[1].
Ruzadolane is a non-narcotic, centrally-acting analgesic agent.
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice[1].
(-)-Aspartic acid is an endogenous NMDA receptor agonist.
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1][2].
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects[1].
LRRK2-IN-8 is a LRRK2 inhibitor. LRRK2-IN-8 inhibits LRRK2 (wt) and LRRK2 (G2019) with IC50s lower than 10 nM, and inhibits TYK2 and NUAK1 with IC50s of 10-100 nM[1].
Secretoneurin, rat, a 33-amino acid polypeptide, is generated by proteolytic processing of secretogranin II (SgII). Secretoneurin, rat induces dopamine release in the rat striatum in vivo and in vitro, and it exerts a very strong chemotactic effect on monocytes and eosinophils but not on granulocytes[1].
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease[1].
Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke[1].
MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain[1].
Autocamtide-3, a 13-amino-acid peptide containing Thr287, is a selective CaMKII (Ca2+/calmodulin-dependent kinase II) (CaMK) substrate[1].
CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
POM1 is a potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1, NTPDase 3 and NTPDase 2 respectively[1]. POM1 inhibits ATP breakdown but also blocks central synaptic transmission, an action independent of NTPDase inhibition[2].
Synaptamide is a potent mediator for neurogenic differentiation of NSCs acting through PKA/CREB activation.Target: in vitro: Synaptamide inhibits forskolin-mediated cAMP production (IC50 =6 μM) in CHO-HCR cells. Synaptamide decreases the viability of the LNCaP and PC3 prostate cancer cell lines (IC50=120-130 μM) grown in media containing 10% fetal bovine serum. [1] Synaptamide is an endogenous DHA metabolite with endocannabinoid-like structure, promotes neurite growth, synaptogenesis and synaptic function. Synaptamide potently induces neuronal differentiation of NSCs. Treatment of NSCs with Synaptamide at low nanomolar concentrations significantly increased the number of MAP2 and Tuj-1 positive neurons with concomitant induction of PKA/CREB phosphorylation. [2]
Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].
IM156 (HL156A), a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model[1][2].
Parapenzolate bromide, an antispasmodic, is an orally active mAChR antagonist. Parapenzolate bromide is an anticholinergic agent[1][2].
Tau Peptide (245-274) (Repeat 1 Domain) is aTau fragment.
MIN-101 is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
Ammonium tetrathiomolybdate(VI) is a copper chelator and also is a class of sulfide donor. Ammonium tetrathiomolybdate(VI) has neuroprotection effects. Ammonium tetrathiomolybdate(VI) can be used for the research of brain ischemia[1].
Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na+ channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively[1]. Remacemide hydrochloride is an anticonvulsant agent[2].
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS)[1].
S-Adenosyl-L-methionine disulfate tosylate is the principal biological methyl donor synthesized in all mammalian cells but most abundantly in the liver.
PD 117519 is an adenosine agonist.Target: Adenosine ReceptorPD 117519 is an adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models[1]. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models[2].
L-Tyrosine-4-13C is the 13C-labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant[1].