TCB2 is an agonist of serotonin 5-HT2A receptor.
5-HT3 antagonist 4 is a 5-HT3 receptor (5HT3R) antagonist. 5-HT3 antagonist 4 prevents diabetes-induced depressive phenotypes in mice[1].
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively[1].
Dihydroergotamine mesylate is an ergot alkaloid used to treat migraines.Target: 5-HT ReceptorsDihydroergotamine is not as effective as sumatriptan or phenothiazines as a single agent for treatment of acute migraine headache; however, when administered with an antiemetic, dihydroergotamine appears to be as effective as opiates, ketorolac, or valproate. Given its nonnarcotic properties, parenteral dihydroergotamine combined with an antiemetic should be considered as effective initial therapy in clinical practice [1]. The introduction of the intranasal formulation of DHE provides both pharmacologic and patient-convenience advantages for use in migraine therapy [2, 3].
Conantokin-T is a γ-carboxyglutamate-containing, N-methyl-D-aspartate (NMDA) antagonist peptidewith an IC50 value of 2 μM. Conantokin-T inhibits NMDA receptor-mediated calcium influx in central nervous system neurons. Conantokin-T can be purified from the venom of the fish-hunting cone snail, Conus tulipa[1].
AJH-836 is an activator of Munc13-1 and PKC ε/α (Kd: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases[1].
TDN345 is a Ca2+ antagonist, used for the treatment of vascular and senile dementia including Alzheimer's disease.
YM-244769 hydrochloride is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].
BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability[1].
(Arg)9 (Nona-L-arginine;Peptide R9) is a cell-penetrating peptide; exhibits neuroprotective activity with an IC50 of 0.78 μM in the glutamic acid model.
PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis of PI3K inhibitor (2-imino-azolinone-vinyl fused-benzene derivative) that can be used for the research of autoimmune disorders, cardiovascular diseases, and neurodegenerative diseases[1].
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research[1][2][3][4].
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.IC50 value: 289 nM(EC50) [2]Target: M1 mAChR agonistin vitro: TBPB activates M(1) through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its unprecedented selectivity. Whole-cell patch-clamp recordings demonstrated that activation of M(1) by TBPB potentiates NMDA receptor currents in hippocampal pyramidal cells but does not alter excitatory or inhibitory synaptic transmission, responses thought to be mediated by M(2) and M(4) [1]. in vivo: TBPB was efficacious in models predictive of antipsychotic-like activity in rats at doses that did not produce catalepsy or peripheral adverse effects of other mAChR agonists [1].
AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke[1].
PEN(mouse) (proSAAS(221-242)) is the precursor of a number of peptides that function as neuropeptides[1].
NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research[1][2].
SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity[1][2]. SB202190 hydrochloride induces autophagy[3].
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.IC50 Value: 151 nMTarget: COMTin vitro: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.in vivo: Levodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. We report four case histories describing clinical experience of using levodopa/carbidopa/entacapone 200/50/200 mg, one of the latest doses of this formulation, in a range of patients with Parkinson's disease. These cases illustrate that levodopa/carbidopa/entacapone 200/50/200 mg provides improvements in symptomatic control.Clinical trial: The combination product carbidopa/levodopa/entacapone (CLE) was approved in 2003 for the treatment of PD patients.
Gomisin N, isolated from Schisandra chinensis, produces beneficial sedative and hypnotic bioactivity. Gomisin N has the potential for use in the treatment of allergy. Gomisin N is an anti-cancer drug candidate capable of inhibiting the proliferation and inducing the apoptosis in cancer[1][2][3].
Galnon TFA is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with Kis of 11.7 and 34.1 μM respectively. Galnon TFA exhibits anticonvulsant and anxiolytic effects[1][2].
VP3.15 dihydrobromide 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 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS)[1].
Lamotrigine-13C,d3 is the 13C- and deuterium labeled. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
3,5-Dihydroxy-2-naphthoic acid is a Naphthoic acid derivative. Naphthoic acid is a NMDA receptor allosteric modulator[1].
Neuropeptide Y(29-64) is a 36 amino acid peptide, a fragment of Neuropeptide Y.
SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier[1].
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin treatment of the malaria parasitesPlasmodium falciparum [1][2].
Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.
Visnagin, an antioxidant furanocoumarin derivative, possess anti-inflammatory and analgesic properties. Visnagin has substantial potential to prevent Cerulein induced acute pancreatitis (AP). Visnagin possess promising vasodilator effects in vascular smooth muscles[1][2].
Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia[1][2][3].
DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM[1]. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity[2].