Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain[1].
AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro[1].
Neuropeptide AF (93-110), Human is an endogenous antiopioid peptide.
Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal systems enhancer for Ro 5-4864-induced convulsions.Target: GABA ReceptorNefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01-0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1-10 μM). Nefiracetam interacts with PKA and PKC pathways, which may explain a cellular mechanism for the action of cognition-enhancing agents. Lower (submicromolar) concentrations of the nootropic Nefiracetam reduces ACh-evoked currents to 30% (0.01 μM) and 38% (0.1 μM) of control after a 10-minute treatment [1].Nefiracetam administered orally inhibits Ro 5-4864-induced convulsions in EL mice. Nefiracetam also efficiently inhibits Ro 5-4864-induced convulsions in DDY mice at doses higher than 10 mg/kg [2]. Nefiracetam administered daily 1 hour before each training session facilitates the acquisition process of the avoidance response [3].
Erenumab is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene–related peptide (CGRP) receptor. Erenumab can be used for the prevention of episodic migraine[1].
Bleformin A is a potent BChE inhibitor with an IC50 value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD)[1].
Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively[1][2].
Myristicine act as a serotonin receptor antagonist, a weak monamine oxidase (MAO) inhibitor. Myristicine is the main component of nutmeg essential oil from Myristica fragrans Houtt. Myristicine abuse produce hallucinogenic effects, organ damage, deliriumand others[1].
(R)-Oxybutynin (Aroxybutynin), a (R)-isomer of Oxybutynin, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin can be used for researching incontinence due to neurogenic bladder dysfunction[1][2][3].
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities[1][2][3].
Dicarbine dihydrochloride blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine dihydrochloride could be used in the schizophrenia and alcoholic psychosis studies[1][2].
Naspm (1-Naphthyl acetyl spermine) trihydrochloride, a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research[1][2][3].
Scopolamine hydrobromide is a high affinity (nM) muscarinic antagonist. 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC50 of 2.09 μM.
CP 226269 is a potent dopamine D4 receptor agonist that induces calcium flux with EC50 of 32.0 nM. CP 226269 can be used in the research of schizophrenia and other related diseases[1].
L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
FAAH/MAGL-IN-4 (Compound 13) is a potent fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitor with IC50s of 9.1 nM and 7.9 μM, respectively. FAAH/MAGL-IN-4 can be used for the research of pain and CNS disorders[1].
Eslicarbazepine acetate, an antiepileptic drug, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
Notoginsenoside R1, the main bioactive component in panaxnotoginseng, is reported to have some neuronal protective, antihypertensive effects. IC50 value:Target:In vitro:In vivo: Notoginsenoside R1 significantly reduce blood pressure in spontaneously hypertensive rats and induce nitric oxide generation through increasing the phosphorylation of iNOS. Notoginsenoside R1 reduces the caudal blood pressure of spontaneously hypertensive rats through induction of iNOS regulated by long non-coding RNA AK094457 [1]. The mice with notoginsenoside R1 treatment showed significant amelioration in the cognitive function and increased choline acetyl transferase expression, as compared to the vehicle treated mice. Notoginsenoside R1 treatment inhibited Aβ accumulation and increased insulin degrading enzyme expression in both APP/PS1 mice and N2a-APP695sw cells [2]. In Notoginsenoside R1 treated rats, expression of TGF-β1and Smad3 at each time point was down-regulated, with statistical significance(P0.05) compared with that in the NDMA group [3].
Phenelzine is a non-selective and irreversible monoamine oxidase inhibitor (MAOI), used as an antidepressant and anxiolytic.
SSR-241586 is an antagonist of neurokinin receptors. SSR-241586 is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS)[1][2].
Glycine-d2 is the deuterium labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
Methylene Violet 3RAX is a phenazine dye to stain the mitochondria of cells. Methylene Violet 3RAX can change the molecular structure of DNA, undermine the module of DNA, and induce the generation of the reactive singlet oxygen. Methylene Violet 3RAX shows inhibition for human erythrocyte AChE and human plasma BChE with an Kis of 1.58, 0.51 μM, respectively. Methylene Violet 3RAX has the potential for the research of potential photosensitizers for mitochondrial targeting action in PDT (photodynamic therapy)[1][2].
3,4-Dihydro Naratriptan is a serotonin 5-HT1-receptor agonist. 3,4-Dihydro Naratriptan exhibits selective vasoconstrictor activity. 3,4-Dihydro Naratriptan can be used for migraine diseases research[1].
Carprofen-13C,d3 is the deuterium and 13C labeled Carprofen[1]. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[2][3][4].
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of cocaine-seeking behavior in rats[1][2][3].
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitory activity on leukotriene biosynthesis, with an IC50 of 12.1 μM[1][2].
Felbamate (FBM) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA) .Target: NMDA ReceptorFelbamate (marketed under the brand name Felbatol by MedPointe) is an anti-epileptic drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drugs usage to severe refractory epilepsy.Felbamate has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptor of relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.
GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia[1][3].