Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation[1].
NLRP3-IN-13 (Compound C77 in reference patent) is a selective and potent NLRP3 inhibitor (IC50: 2.1 μM). NLRP3-IN-13 inhibits NLRP3 andNLRC4 inflammasomes, and inhibits NLRP3-mediated IL-1β production. NLRP3-IN-13 also inhibits NLRP3 ATPase activity. NLRP3-IN-13 can be used in the research of neuroinflammatory disorders[1].
Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class.
Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice [1].
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1].
Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively[1].
Lu AA33810 is a potent and selective antagonist of neuropeptide Y5 receptor with a Ki of 1.5 nM for the human receptor. Lu AA33810 exhibts antianxiolytic-like and antidepressant-like effects[1].
Prifinium bromide is antimuscarinic agent with antispasmodic, antiemetic effect[1].
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively[1][2].
DQP-26 is a potent NMDAR negative allosteric modulator with IC50 values of 0.77 μM and 0.44 μM for GluN2C and GluN2D, respectively. DQP-26 has the potential for NMDAR-associated neurological disease research[1].
Tezosentan-d4 (RO 610612-d4) is the deuterium labeled Tezosentan. Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively[1][2].
Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
N6-[2-(4-Aminophenyl)ethyl]adenosine is a potent, non-selective A3 adenosine receptor agonist.Target: Adenosine receptor agonist.in vitro: N6-[2-(4-Aminophenyl)ethyl]adenosine is a non-selective agonist of the adenosine A3 receptors, at the subprotective dose of 1 mg/kg against electroconvulsions, significantly potentiates the anticonvulsive action of phenobarbital, diphenylhydantoin and valproate against maximal electroshock, being ineffective at lower doses. N6-[2-(4-Aminophenyl)ethyl]adenosine (0.0039-1 mg/kg) also enhances the protective activity of carbamazepine. N6-[2-(4-Aminophenyl)ethyl]adenosine at low doses potentiates the protective activity of Carbamazepine most likely through the A subtype of adenosine receptors. At higher doses, N6-[2-(4-Aminophenyl)ethyl]adenosine seems to enhance the anticonvulsive effect of other antiepileptics via adenosine A1 receptors. [1]in vivo: N6-[2-(4-Aminophenyl)ethyl]adenosine (2-4 mg/kg) has no significant effect on seizure parameters (seizure severity, seizure duration and afterdischarge duration) in amygdala-kindled rats. N6-[2-(4-Aminophenyl)ethyl]adenosine is combined with antiepileptic drugs administered at doses ineffective in fully kindled rats.[2]
(R)-Oxiracetam is the (R)-enantiomer of the nootropic drug oxiracetam. Oxiracetam (ISF 2522) is a nootropic drug of the racetam family and stimulant.IC50 value:Target: nootropic drugOxiracetam (ISF 2522) is a nootropic drug of the racetam family and stimulant.[1][2] Several animal studies suggest that the substance is safe even when high doses are consumed for a long period of time.[medical citation needed] However, the mechanism of action of the racetam drug family is still a matter of research. Oxiracetam is not approved by Food and Drug Administration for any medical use in the United States.
PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.IC50 value:Target: GABA receptorAcamprosate, or N-acetyl homotaurine, is an N-methyl-D-aspartate receptor modulator approved by the Food and Drug Administration (FDA) as a pharmacological treatment for alcohol dependence.Acamprosate has low bioavailability, but also has an excellent tolerability and safety profile. In comparison with naltrexone and disulfiram, which are the other FDA-approved treatments for alcohol dependence, acamprosate is unique in that it is not metabolized by the liver and is also not impacted by alcohol use, so can be administered to patients with hepatitis or liver disease (a common comorbid condition among individuals with alcohol dependence) and to patients who continue drinking alcohol.
Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants.
Paeonol-d3 is the deuterium-labeled Paeonol (HY-N0159)[1].
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects[1][2][3].
Dynamin inhibitory peptide competitively blocks binding of dynamin to amphiphysin, thus preventing endocytosis. Dynamin inhibitory peptide blocks the dopamine D3 effect on GABAA receptors[1].
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6[1].
γ3-MSH is derived from the N-terminal segment of pro-opiomelanocortin (POMC). γ3-MSH stimulates aldosterone secretion by human adrenal tumor cells in culture[1].
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity[1].
Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro[1].
Asenapine maleate, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
[Lys5,MeLeu9,Nle10]Neurokinin A(4-10) (LMN-NKA), an analogue of Neurokinin A, is a selective and potent NK2R agonist. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) has prokinetic activity. [Lys5,MeLeu9,Nle10]Neurokinin A(4-10) can be used to study the roles of the NK-2 receptor in smooth muscle contraction in numerous tissues[1][2][3].
NCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases[1].
Azamethiphos is an organophosphate insecticide and a neurotoxic agent, causing acetylcholinesterase (AChE) inhibition[1].