Droxidopa-13C2,15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis[1][2][3].
Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder[1].
JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research[1].
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway[1].
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist[1].
(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].
Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a Ki of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.
Pheniprazine hydrochloride is a potent and long acting inhibitor of monoamine oxidase. Pheniprazine has the potential for the research of depression[1].
(R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) is an anticholinergic agent. (R,R)-Glycopyrrolate ((R,R)-Glycopyrronium (bromide); (R,R)-Glycopyrrolate (bromide)) has the ability to reduce the frequency of drooling in vivo with developmental disabilities[1].
Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α，5-HT1β and 5-HT2，respectively. Spiroxatrine (R 5188) has a sedative effect[1][2][3][4].
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity[1].
Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction[1][2].
BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity[1][2].
Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties[1][2].
Isoguvacine hydrochloride is a GABA receptor agonist.
Neuropeptide Y (13-36), porcine is a selective neuropeptide Y2 receptor agonist[1].
2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine is a pharmaceutically active compound which is a nootropic agent that acts as cholinesterase inhibitor and is used in treatment of Alzheimer disease[1].
Anagyrine ((-)-Anagyrine) hydrochloride is a quinolizidine alkaloid that has been found in Lupinus albus. Anagyrine hydrochloride binds to muscarinic and nicotinic acetylcholine receptors with IC50 values of 132 and 2096 µM respectively. Anagyrine hydrochloride is a potent and effective desensitizer of nAChR, and Anagyrine hydrochloride can directly, without metabolism, desensitize nAChR[1][2][3].
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively[1].
GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases[1].
Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.
RS-0466, a neuroprotective compound, inhibits β-amyloid-induced cytotoxicity. RS-0466 can be used for research of Alzheimer’s disease[1].
D-Galactose is a natural aldohexose and C-4 epimer of glucose.
4-(6-Bromo-2-benzothiazolyl)benzenamine is a β-amyloid PET (positron emission tomography) tracer that can be used in the diagnosis of neurological diseases, such as Alzheimer's and Down's syndrome.
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also a selective ligand of the GPR35 receptor.
KW-6055 is a benzylpyridine derivative and has anti-amnesic activity.
[Lys8] Vasopressin Desglycinamide is a vasopressin analog, used for the maintenance of active and passive avoidance behavior. [Lys8] Vasopressin Desglycinamide facilitates memory consolidation processes[1].
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells[1].