α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases[1].
Tetanus toxin (830-843) a powerful neurotoxin that reaches by retroaxonal transport and transcytosis the cytoplasm ofspinal inhibitory intemeurons and blocks their ability to release neurotransmitters[1].
L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.Target: NMDA ReceptorL-701324 is a potent, active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents. L-701324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia. L-701324 (2.5-40 mg/kg, i.p.) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg, i.p.).
NSI-189 is a nootropic and neurogenic research chemical derived from nicotinamide and pyrazine.IC50 value:Target: in vitro: NSI-189 has been shown to stimulate neurogenesis of human hippocampus-derived neural stem cells in vitro and in vivo. The hippocampus is responsible for the consolidation of information from short-term memory to long-term memory, along with spatial navigation [1] [2].in vivo: NSI-189 has been shown to increase the hippocampal volume of healthy adult mice by 20% [3].
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model[1][2][3].
Tropatepine is an anticholinergic muscarinic antagonist and can be used as an antiparkinsonian agent[1]. Tropatepine is used to combat against extrapyramidal syndrome induced by neuroleptic drugs[2].
Pramipexole-d5 is the deuterium labeled Pramipexole[1]. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[2][3][4].
Ramelteon is a highly potent and selective melatonin receptor agonist with Ki values of 14 and 112 pM for human melatonin1 and melatonin2.
NAS-181 is a potent and selective rat 5-hydroxytryptamine1B (r5-HT1B) antagonist with an Ki value of 47 nM. NAS-181 increases the 5-HTP accumulation in rat brain regions[1].
Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine.
Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease[1][2][3].
Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Kiapp: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases[1].
Methoxamine hydrochloride is a noradrenergic α1 agonistsup>[1].
Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
Glycine-1-13C is the 13C-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.
ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.
Isospaglumic acid is a neuropeptide found in millimolar concentrations in brain.
Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively[1].
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research[1].
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
BiP inducer X, a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78, is an effective ER (endoplasmic reticulum) stress inhibitor. BiP inducer X preferentially induces BiP with slight inductions of GRP94, calreticulin, and C/EBP homologous protein. BiP inducer X protects neurons from ER stress[1][2].
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease[1].
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI)[1][2].
PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. TRPM8, also known as the cold and menthol receptor 1 (CMR1), is a member of the melastatin subfamily. PF-05105679 is used for clinical efficacy in cold-related pain[1].
A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
CNQX (FG9065) is a potent AMPA/kainate receptor antagonist.
SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.IC50 Value: 4.4 nM ( Ki for hNK-3 receptor); 250 nM( Ki for hNK-2 receptor) [1]Target: NK3 Receptorin vitro: SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1].in vivo: In mice oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1].