Neurological Disease

Cirsimaritin binds weakly to the benzodiazepine site on GABA_A receptors, with antidepressant, anxiolytic and antinociceptive activities.

Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade (IC₅₀=9.8 μM).

Cannflavin B is a flavonoid compound that can be isolated from Cannabis sativa L. Cannflavin B is inhibitors of PGE₂ release (IC₅₀: 0.7 μM), mPGES-1 (IC₅₀: 3.7 μM), and 5-lipoxygenase. Cannflavin B has multiple activities such as anti-inflammatory, antioxidant, anti-glycation, anti-ferroptosis, anti-tumor, and anti-Leishmania (IC₅₀: 14 μM). Cannflavin B can also inhibit the TrkB-BDNF signaling pathway.

GR 103691 is a potent, selective dopamine D₃ receptor antagonist with a K_i value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D₃ over hD₄ and hD₁ sites.

Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.

Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP₄₅₀). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.

TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC₅₀ of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain.

NEK7 degrader-1 is a NEK7 molecular glue degrader with a DC₅₀ of 9  nM. NEK7 degrader-1 dose-dependently inhibits caspase-1 activity and IL-Ιβ release in macrophages in response to NLRP3 inflammasome activation. NEK7 degrader-1 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research.

Biotin-β-Amyloid (1-42), human TFA (Biotin-Amyloid β-Peptide (1-42) (human) TFA) is the botin labeled β-Amyloid (1-42), human TFA (HY-P1363). β-Amyloid (1-42), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.

DS2 is a selective positive allosteric modulator of δ-GABA_A receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.

TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC₅₀ value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain.

Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H₃-receptor, with an IC₅₀ of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.

Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.

Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.

Substance P(1-7) TFA is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) TFA gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.

DQP-1105 is a potent noncompetitive NMDA receptor antagonist. DQP-1105 inhibits GluN2C- and GluN2D-containing receptors (IC₅₀=7.0 and 2.7 μM, respectively). The IC₅₀ values are at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors.

Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.

Alizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders.

6-Methylflavone is an activator of α₁β₂γ_2L and α₁β₂ GABA_A receptors.