Neurological Disease

(R,S,S)-Dihydrotetrabenazine (R,S,S-DHTBZ) is a kind of discrete isomeric secondary alcohol metabolites of Tetrabenazine (TBZ, HY-B0590), is a poor VMAT2 inhibitor (K_i = 690 nM).

NPC-15437 dihydrochloride is a selective, penetrable and reversible protein kinase C (PKC) inhibitor, with an IC₅₀ of 19 μM. NPC-15437 dihydrochloride interferes with mechanisms underlying memory consolidation.

Emicerfont is a corticotropin-releasing factor type 1 (CRF₁) receptor antagonist with an IC₅₀ of 66 nM.

Entacapone-d₁₀ is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC₅₀ values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC₅₀s>50 μM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC₅₀ of 3.5 μM, can be used for the research of metabolic disorders.

Robalzotan hydrochloride (NAD-​299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.

Antidepressant agent 1 is a pyrazidole-halogeno-derivative with antidepressant effects. Antidepressant agent 1 also can be used to increase body temperature.

MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a K_i of 0.67 nM for rat mGluR5. MFZ 10-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Merinetug is a humanized IgG1κ antibody targeting Amyloid beta/Aβ. The corresponding isotype control is: Human IgG1 kappa, Isotype Control (HY-P99001).

A-381393 is a potent, selective, brain penetrate dopamine D₄ receptor antagonist, with K_is of 1.5, 1.9 and 1.6 nM for human dopamine D_4.4, D_4.2, and D_4.7 receptor, respectively, >2700-fold selectivity over D₁, D₂, D₃ and D₅ dopamine receptors. A-381393 shows moderate affinity for 5-HT_2A (K_i, 370 nM).

FAM labled Nusinersen sodiumis a FAM labled Nusinersen sodium.

Atropine-d₅ is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.

KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC₅₀ 0.21 nM in Neuro2A cells.

Zylofuramine is a psychomotor stimulant. Zylofuramine can be used in the research related to appetite suppressants and Alzheimer's disease.

Cyprodime is a selective μ opioid receptor (MOR) antagonist with K_is of 5.4, 244.6, and 2187 nM for μ, δ, and κ, respectively.

DORA-22 is an orally active dual orexinergic receptor antagonist, and improves the sleep disruption and memory impairment. DORA-22 can be used for study of insomnia.

(-)-5-HT2C agonist-3 (compound (-)-19) is a 5-HT_2C selective agonist with G_q signaling preference, with EC₅₀ values for 5-HT₂ receptors of 5-HT_2C: 103 nM; 5-HT_2B: 570 nM; 5-HT_2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research.

Leptomerine, an alkaloid from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer Disease. Leptomerine inhibits acetyl cholinesterase (AChE) with an IC₅₀ of 2.5 μM. Anticholinesterasic activity.

NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a K_i value of 4 nM and a pK_i value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC₅₀ values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects.

Guanethidine sulphate was synthesized in 1959. Guanethidine is thought to lowing blood pressure by interfering with the metabolism of chemical transmitter substances in post-ganglionic sympathetic nerve fibres.

MFZ 2-13 (O-456) is an N-demethylated intermediate and N-nor-analogue of MFD 2-12. MFZ 2-13 inhibits dopamine uptake through the human dopamine receptor with an IC₅₀ of 1.4 nM.