Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19[1][2][3][4][5].
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity[1][2].
WAY-213613 is a potent, selective human EAAT2 inhibitor (IC50, 85 nM), exhibits 59- and 45-fold selectivity over human EAAT1 and EAAT3. Inhibits glutamate uptake in rat cortical synaptosomes[1].
Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica[1].
Batroxobin (DF-521) is a snake venom that can be obtained from Bothrops atrox moojeni. Batroxobin promotes thrombolysis, prevents the recurrence of thrombus, and provides neuroprotection. Batroxobin has the potential for the research of cerebral venous thrombotic diseases[1].
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM[1].
NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons[1].
Moguisteine(BBR-2173) is a novel peripheral non-narcotic antitussive drug.Target: OthersMoguisteine is a novel peripheral nonnarcotic antitussive agent that has proved to be as active as codeine in several experimental models of induced cough in guinea-pigs and dogs. It acts neither through the opiate receptors nor on the cough centre, and its action is possibly mediated by the interaction with rapidly adapting irritant receptors along the tracheobronchial tree. In controlled clinical trials, moguisteine has been shown to be safe and to effectively reduce cough associated with such respiratory disorders as acute upper respiratory tract infection, chronic bronchitis, pulmonary fibrosis and malignancies [1, 2].
CGP 54626 (hydrochloride) is a selective antagonist of GABAB receptor with an IC50 value of 4 nM. CGP 54626 (hydrochloride) can be used to investigate the role of GABAB receptors in neurological signaling[1].
Scheffoleoside A is a neuroprotective agent can be derived from Centella asiatica. Scheffoleoside A exhibits moderate activity in inhibiting 6-OHDA-induced cytotoxicity[1].
Olivetol-d9 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activi
Hexafluorenium dibromide (Mylaxen) is a potent cholinesterase (ChE) inhibitor with pI50 value of 6.96 and Ki value of 2.4 nM for human plasma cholinesterase (ChE)[1].
mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic[1].
Pancopride is a new potent and selective 5-HT3 receptor antagonist.
Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.Target: Potassium ChannelDoxapram is a respiratory stimulant. Doxapram (15-150 microM) also evoked 3H overflow in a concentration dependent manner, and doxapram-evoked release was inhibited by the Ca2+ channel blocker nifedipine (5 microM). Analysis of released tritiated compounds suggested that doxapram preferentially stimulated the release of dopamine. Our results indicate that the mechanism of action of doxapram shares similarities with that of hypoxia in the carotid body [1]. Doxapram (1-100 microM) caused rapid, reversible and dose-dependent inhibitions of K+ currents recorded in type I cells (IC50 approximately 13 microM). doxapram was also seen to directly inhibit Ca(2+)-independent K+ currents. Doxapram was a more potent inhibitor of the Ca(2+)-activated K+ currents recorded under control conditions. Doxapram (10 microM) was without effect on L-type Ca2+ channel currents recorded under conditions where K+ channel activity was minimized and was also without significant effect on K+ currents recorded in the neuronal cell line NG-108 15, suggesting a selective effect on carotid body type I cells. The effects of doxapram on type I cells show similarities to those of the physiological stimuli of the carotid body, suggesting that doxapram may share a similar mechanism of action in stimulating the intact organ [2].
[Ala9,10, Lys11,12] Glycogen Synthase (1-12) is a selective substrate for phosphorylation by protein kinase C (PKC). [Ala9,10, Lys11,12] Glycogen Synthase (1-12) can be used to determine the activity of protein kinase C[1].
Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury[1][2][3].
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
FCPR03 is a novel potent, selective PDE4 inhibitor with IC50 of 60, 31 and 47 nM for PDE4CAT (PDE4 catalytic domain), PDE4B1 and PDE4D7, respectively; displays >2,000-fold selectivity over other PDEs; effectively increases the production of cAMP, promotes CREB phosphorylation, and inhibits NF-κB activation both in vitro and in vivo; displays anti-neuroinflammation potential, promising antidepressant-like effects in vivo.
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils[1].
(Phe13,Tyr19)-MCH (human, mouse, rat) is a potent SLC-1 and S643b receptor ligand. (Phe13,Tyr19)-MCH (human, mouse, rat) can be used as an agonist for SLC-1 and S643b receptor[1].
M4 mAChR agonist-1 (compound 10a) is a potent M4 mAChR agonist with an EC50 >10 μM for human M4[1].
D-Tetramannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Tetramannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
w-Conotoxin SVIB is a peptide toxin, it can be isolated from Conus venoms. w-Conotoxin SVIB inhibits twitch response with an IC50 value of 37 nM. w-Conotoxin SVIB induces respiratory distress and it can be lethal to mice at a high concentration[1][2].
PF-06447475 trihydrochloride is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 trihydrochloride can be used for parkinson's disease (PD) research[1].
Head activator neuropeptide is a mitogen for mammalian cell lines of neuronal or neuroendocrine origin. Head activator neuropeptide signals by binding GPR37 and stimulates cells to enter mitosis[1].
Dihydroactinidiolide, existing in plant leaves and fruits, is a potent plant growth inhibitor, a regulator of gene expression and is responsible for photo acclimation in Arabidopsis. Dihydroactinidiolide has antioxidant activity, antibacterial activity, anticancer activity and neuroprotective effect[1].
Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively[1][2][3].