Neurological Disease

Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough.

TP-030-1, a chemical probe, is an inhibitor of RIPK1. TP-030-1 inhibits hRIPK1 with a K_i value of 3.9 nM and inhibits mRIPK1 with an IC₅₀ value of 4.2 μM. TP-030-1 can be used for the research of inflammatory diseases and neurodegenerative diseases.

Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems.

NNMT-IN-5 (Compound 3-12) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC₅₀ = 47.9 ± 0.6 nM). NNMT-IN-5 also has an excellent selectivity profile over a panel of human methyltransferases. NNMT-IN-5 can be used for the research of cancer, diabetes, metabolic disorders, and neurodegenerative diseases.

Arnica oil can be used to relieve symptoms of inflammation and pain.

Molindone ((±)-Molindone), an indole derivative, is a potent dopamine D2 and D5 receptor antagonist. Molindone ((±)-Molindone) can be used for the research of schizophrenia and severe mental illness.

FTO-IN-4 is a potent and selective inhibitor of fat mass obesity-associated protein (FTO).

Altissimacoumarin F (Compound 4) is a terpenylated coumarin. Altissimacoumarin F can be isolated from the stem bark of Ailanthus altissima. Altissimacoumarin F enhances SIRT1 activity, decreases p53 transcriptional activity. Altissimacoumarin F can be used for the research of age-related disorders.

E3 ligase Ligand 29-azacyclohexane-O-cyclohexane-CO is a synthesized E3 ligase ligand-linker conjugate that can be used to synthesize PROTAC LRRK2 Degrader-3 (HY-178797). PROTAC LRRK2 Degrader-3 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.

Cholesterol (from plant) is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol (from plant) plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol (from plant) is also an endogenous estrogen-related receptor α (ERRα) agonist.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

1(S)-Tetrahydrocannabidiphorol is a drug analogue and can be used for the research of neurological disease.

7(Z)-Pentacosene is an aggregation pheromone of the European earwig (Forficula auricularia). 7(Z)-Pentacosene can be used in the study of insect behavior and neurobiology.

[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pK_i of 10.68 and a pEC₅₀ of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

ORL1 antagonist 2 (1B) is an opioid receptor-Like 1 (ORL1) antagonist, usd in P-glycoprotein (P-gp) research.

GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC₅₀s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.

SM 10888 is a selective and orally active cholinesterase (ChE) inhibitor. SM 10888 can increase brain acetylcholine release. SM 10888 can be used for the research of neurological disease, such as Alzheimer's disease.

GABAB receptor antagonist 5 (Compound 23) is a competitive GABA_B receptor antagonist. GABAB receptor antagonist 5 is promising for research of neuropsychiatric diseases, such as epilepsy, depression, and addiction.

sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD).

NX210 is a dodecapeptide derived from the SCO-spondin protein. NX210 can increase cell survival and induce neurite outgrowth, and participate in cell-cell and cell-matrix interactions. NX210 can be used in research on spinal cord injury recovery.