Bryonolic acid is an active triterpenoid compound with immunomodulatory, anti-inflammatory, antioxidant and anticancer activities[1][2][3].
Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia, cocaine addition, and obesity[1][3].
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse[1]. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis[2].
Neuropathiazol is a synthetic small molecule that induces neuronal differentiation of adult hippocampal neural progenitor cells.
Ansofaxine is a serotonin-norepinephrine reuptake inhibitor (SNRI) used for the research of depression[1].
HQ-415 is a class of clinically relevant bioactive metal chelators related to clioquinol. The effective concentration eliciting a EC50 for HQ-415 is 15 μM. IC50 value: 15 μM (EC50)in vitro: In TDP-43-expressing cells, CQ fails to synergize with HQ-161 and actually antagonizes HQ-161 rescuing activity. In contrast, despite the fact that CQ was completely inactive against TDP-43, it strongly synergized with HQ-415, decreasing the EC50 from 16 to 5 μM. HQ-415 is active in the TDP-43 model, but CQ was not HQ-161 and HQ-415 are retested in dose for their ability to rescue TDP-43. Both HQ-161 and HQ-415 rescue TDP-43 toxicity. In cells expressing α-syn, HQ-161, despite being inactive on its own, synergized with HQ-415, reducing the EC50 from 21 to 14 μM. HQ-415 strongly synergizes with CQ at multiple concentrations in cells expressing α-syn.
(S,S)-BD-AcAc 2 ((S,S)-Ketone Ester) is a (S,S)-enantiomer of BD-AcAc 2. BD-AcAc 2 elevates the AcAc and acetone levels, thereby produces sustained ketosis and significantly delays central nervous system oxygen toxicity (CNS-OT) seizures[1].
Hydroxyl-γ-isosanshool is one of the major alkylamides in Z. bungeanum and Z. schinifolium oils. Hydroxyl-γ-isosanshoo induces a numbing and anesthetic sensation[1].
Exoenzyme C3, clostridium botulinum is a promising agent to inactivate RhoA in neurons due to preventing the detrimental effect of active Rho in the recovery of injured neuronal systems. Exoenzyme C3, clostridium botulinum is used for the study of post-traumatic neuro-regeneration[1].
BMT-090605 (BMT 090605, BMT090605) is a potent, selective adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 0.6 nM; weakly inhibits BIKE and GAK with IC50 of 45 and 60 nM, respectively.
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively[1].
Isodihydrofutoquinol B (compound 9), an active compound, can be isolated from the stems of Piper kadsura (Choisy) Ohwi. Isodihydrofutoquinol B has A neuroprotective effect on Aβ25-35-induced PC12 cell damage with E50 values of 3.06-29.3μM[1].
PPDA is a subtype-selective NMDA receptor antagonist that preferentially binds to NR2C/NR2D containing receptors[1].
ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ. IC50 value: Target: AβThis potent post-transcriptional modulation of APP expression differs from other mechanisms such as inhibition of secretases. Secretase inhibitors have been pursued as disease modifying strategies by a number of pharmaceutical firms but they have encountered numerous setbacks during clinical development. ARN2966 is non toxic, orally absorbable, blood-brain-barrier penetrable, and effective in vitro and in vivo.
α-Methyl-DL-aspartic acid is a specific inhibitor of argininosuccinate synthase (ASS), and also is the rate-limiting enzyme for the recycling of 1-citrulline to 1-arginine[1].
Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].
Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research[1].
Purmorphamine is a smoothened receptor agonist with an EC50 of 1 μM.
RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively[1][2].
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].
BuChE-IN-4 (Compound C6) is a potent inhibitor of BuChE with an IC50 of 7.7 nM. BuChE-IN-4 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity[1].
JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively; attenuates IL-1β release with pEC50 of 6.7 (human blood), 7.5 (human monocytes) and 7.1 (rat microglia); exhibits target engagement in rat brain with brain EC50 of 78 ± 19 ng/ml, as well as functional block of Bz-ATP induced IL-1β release; attenuateas amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease[1].
9-Cyclopentyladenine monomethylsulfonate (9-CP-Ade mesylate) is a stable non-competitive adenylate cyclase inhibitor with cell permeable properties[1][2].
[D-p-Cl-Phe6,Leu17]-VIP is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor, with the IC50 of 125.8 nM. [D-p-Cl-Phe6,Leu17]-VIP has no activity on glucagon, secretin or GRF receptors[1][2][3].
PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator; exhibits functional selectivity for receptors containing α2/3/5 subunits, with significant positive allosteric modulation (90-140%) but negligible activity (<20%) at GABAA receptors containing α1 subunits; demonstrates a robust increase in saccadic peak velocity, increases in beta frequency qEEG and a slight saturating increase in body sway in clinical trials. Epilepsy Phase 1 Clinical
Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia (extracted from patent US20150290125A1/US20110091459A1)[1][2].
Ginkgolide K, isolated from Ginkgo biloba, induces protective autophagy through the AMPK/mTOR/ULK1 signaling pathway. Ginkgolide K possesses neuroprotective activity[1].
Sch412348 is a potent competitive antagonist of the human adenosine A2A receptor (Ki=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.
Nocistatin (human) blocks nociceptin-induced allodynia and hyperalgesia, and attenuates pain evoked by prostaglandin E2[1].