Nialamide is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class that was used as an antidepressant.
Thioridazine is an antipsychotic drug, used in the treatment of schizophrenia and psychosis, shows D4 selectivity or serotonin antagonism.
PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[1].
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities[1][2][3][4][5].
A2A receptor antagonist 1 is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.IC50 Value: 33 nM(EC50)Target: mGluR5in vitro: VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration?response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. in vivo:
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively[1]. 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage[2].
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis[1][2].
(E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model[1].
Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].
(R)-Baclofen(STX209) is a selective GABAB receptor agonist. IC50 value:Target: GABAB receptorGABAB receptors are metabotropic receptors which produce slow inhibitory signals. By manipulating GABAB receptor activity using Baclofen, a variety of functions are studied including synaptic transmissions and antinociception events.
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT[1][2]. Metoprine is an antifolate and antitumor agent[3].
Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
Piperylone can be used as an antispasmodic.
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2].
A Zn2+-dependent pan-inhibitor of class I and class II HDACs with a long half-life (12h) in vivo; significantly enhances the migration of astrocytes and accelerates wound repair more effectively than SAHA and VPA; up-regulates the expression of NGF, phospho-TrkA, p-AKT, NF-κB, and Bcl-2, while down-regulates the expression of p75 NTR, phospho-JNK, and Bax.
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases[1].
Neuroinflammatory-IN-2 (compound 7i) is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease[1].
Deudextromethorphan (AVP-786) hydrobromide hydrate is a deuterated form of dextromethorphan/quinidine (AVP-923, Nuedexta). Deudextromethorphan hydrobromide hydrate, a glutamate-targeting agent, is an orally active N-methyl-D-aspartate (NMDA) receptor antagonist. Deudextromethorphan hydrobromide hydrate can be used for the research of Pseudo-Bulbar Affect, traumatic brain injury, behavioral disinhibition and agitation in AD[1][2][3].
Tominersen (RG6042) is a second-generation 2′-O-(2-methoxyethyl) antisense oligonucleotide that targets huntingtin protein (HTT) mRNA and potently suppresses HTT production. Tominersen can be used for the research of Huntington’s disease[1].
SORT-PGRN interaction inhibitor 2 is a SORT-PGRN inhibitor that can decreases SORT1 protein expression and increases extracellular PGRN secretion in mammalian cell lines. SORT-PGRN interaction inhibitor 2 can be used for neurological disease research[1].
6-Epiagarotetrol is a neuroprotective agent can be extracted from Aquilaria sinensis. 6-Epiagarotetrol has a protective effect on corticosterone-induced PC12 cell damage[1].
ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively)[1].
Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation[1][2].
CGS 21680 is a specific adenosine A2A receptor agonist, used for treatment of neurological disease.
BMS-901715 (BMS901715) is a potent, selective adapter protein-2 associated kinase 1 (AAK1) inhibitor.
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect[1].
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
Scopine Hcl salt is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.