Neuroscienza

Aplindore Fumarate (DAB-452), a selective dopamine D2/D3 partial agonist, is used in Parkinson's and schizophrenia research.

Litoxetine: a selective 5-HT inhibitor & 5-HT3 antagonist, used as an antidepressant with antiemetic effects, Ki=85 nM.

AZD 9272 is a brain-permeable mGluR5 antagonist for the study of gastroesophageal reflux.

L-838417 is a GABAA receptor subtype-selective benzodiazepine site-selective ligand and GABAA receptor-positive modulator used in the study of anxiety disorders

H-9 dihydrochloride: Strong PKA inhibitor, curbs 5-HT response and EGF signaling, affects pharyngeal function.

5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

GSK233705, a muscarinic antagonist, is used to prevent/treat COPD and asthma.

CP-810123 is an α7 nAChR agonist used to treat cognitive deficits associated with psychiatric or neurological disorders such as schizophrenia.

Teniloxazine is an orally available antidepressant compound with anti-hypoxic properties.

Agomelatine HCl is a MT1/MT2 receptor agonist (Ki: 0.1-0.27 nM) and a 5-HT2C antagonist (pKi: 6.2-6.4).

DMCM hydrochloride is a non-selective fully inverse agonist of benzodiazepine.

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of

Pimethixene maleate (Pimetixene maleate) is a 5-HT2B receptor antagonist with sedative activity that can be used to study dry cough in children.

Piromelatine is an agonist of melatonin MT1/MT2 receptors, 5-HT1A and 5-HT1D, and an antagonist of 5-HT2B.Piromelatine has antinociceptive activity with

NB001 (HTS 09836) is an inhibitor of adenyl cyclase 1 exhibiting effects on neural and non-neural pain.

Riluzole hydrochloride, an anticonvulsant Na+ channel blocker, inhibits GABA uptake (IC50: 43 µM).

Suriclone (RP 31264), a cyclic pyrrolidone for anxiety, modulates GABA-A receptors without major sedation.

MNI 137 is a negative allosteric modulator of mGlu2. MNI 137 inhibits glutamate-induced calcium mobilization with IC50s of 8.3 and 12.6 nM for human and rat.

Anpirtoline hydrochloride (D-16949 hydrochloride) is a 5-HT1B receptor agonist and 5-HT3 receptor antagonist used in the study of dyskinesia.

Otenzepad (AF-DX 116) is a selective antagonist of M2 mAChR with IC50s of 386 nM and 640 nM for rat heart and rabbit peripheral lung.

Nerisopam is an agonist of gamma-aminobutyric acid (GABA) receptor.

CBiPES hydrochloride (CBiPES HCl) is an orthosteric modulator of the mGlu2 receptor and is used to study neurological disorders like epilepsy.

ADR-851 free base is an antagonist of the HT3 receptor.

Sarizotan HCl (EMD 128130 HCl) is a 5-HT1A receptor and dopamine receptor agonist and an hERG channel inhibitor used in Parkinson;s disease research.

Tiospirone (BMY 13859-1 free base) is a 5-HT2 receptor antagonist and a dopamine blocker used in the study of neurological disorders such as schizophrenia.

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist, has weak α1 adrenoceptor blocking activity.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

ASM-024, a synthetic piperazine, activates nicotinic and β2-adrenergic receptors for potential asthma and bronchitis treatment with anti-inflammatory effects.

LSN2463359 is a positive allosteric modulators of the mGlu5 receptor.

Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor (IC50: 0.5 μM) that can be used to study neurological disorders.

Ru-32514 is a benzodiazepine receptor agonist.

LY-2300559 is an agonist of metabotropic glutamate receptor 2 (mGluR2) and can be used in studies about the treatment of migraine.

Goxalapladib（GSK 677116） is a small molecule compound that can be used to treat cardiovascular risks associated with atherosclerosis.

RS 67333 hydrochloride is a selective 5-HT4R partial agonist (pKi=8.7) with neuroprotective properties for Alzheimer's research.

Buntanetap ((+)-Phenserine) is an inhibitor of TINAPs used in the study of neurological disorders, endocrine and metabolic disorders, and cardiovascular disease

PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases.

Dipraglurant: a blood-brain permeable mGluR5 NAM, orally active, selective, IC50 = 21 nM, treats PD-LID.

CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of mGluR1b

CGP 55845: potent, selective GABAB blocker, IC50=5 nM, hinders agonist binding, reduces GABA/glutamate release.

NAS-181 free base is a 5-HT(1B) receptor antagonist.

6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.

PQM130 is a Feruloyl-Donepezil Hybrid compound against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity.

MAO-B-IN-27 (Compound 12c), a monoamine oxidase B (MAO-B) inhibitor, exhibits a potent and selective inhibitory effect on hMAO-B, with an IC50 value of 8.9 nM,

LY2033298 enhances oximoline's effect on hamster circadian rhythms, aiding neurosystem disorders.

Flesinoxan HCl is the salt form of Flesinoxan, which is a selective 5-HT1A receptor agonist.

Tiotropium Bromide hydrate is a potent, long-lasting anticholinergic bronchodilator for COPD, with high affinity for muscarinic receptors M1, M2, and M3.

BACE1-IN-10 is a potent inhibitor of BACE1, demonstrating sub-micromolar activity against recombinant BACE1 (rBACE1) [1].

QM-FN-SO3 is a blood-brain barrier (BBB)-penetrable, near-infrared (NIR) probe with aggregation-induced emission (AIE) activity, specifically designed for the detection of Aβ plaques. It exhibits ultra-high signal-to-noise (S/N) ratio, binding affinity, and high-performance NIR emission, making it suitable for in vivo detection of Aβ plaques [1].

MAO-B-IN-13: a potent, reversible MAO-B inhibitor with BBB penetration, neuroprotective effects; used in Parkinson’s research (IC50=10nM).

Capeserod HCl, a 5-hydroxytriptamine 4 (5-HT4) receptor agonist, is used potentially for the treatment of Alzheimer's disease.

1CAY10649, a thiazolinone compound, directly inhibits 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) with an IC50 value of 0.28 μM and in a soluble fraction of an S100 PMNL cell lysate with an IC50 value of 0.09 μM, following stimulation by calcium and arachidonic acid. This activity highlights its potential in mitigating inflammatory responses by targeting the biosynthesis of leukotrienes, substances implicated in various inflammatory processes such as neutrophil chemotaxis, increased vascular permeability, and smooth muscle contraction.

JNJ-46281222: mGlu2-selective, potent PAM, Kd = 1.7 nM, pEC50 = 7.71.

LG 50643 is a muscarinic antagonist.

Velusetrag(TD-5108), a potent 5-HT4 agonist, is in development for gastroparesis, constipation, and IBS.

FPTQ is a highly effective antagonist of mGluR 1, displaying IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively [1].

rTRD01 is a TDP-43 ligand that selectively binds to the RRM1 and RRM2 domains of TDP-43, exhibiting a dissociation constant (Kd) of 89 µM for TDP-43 102–269.

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

NCS-382 (sodium) is a potent antagonist of the GABA receptor, exhibiting anti-sedative and anti-hypnotic properties, with applications in neurological disease

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM.

L 687306 is a partial agonist of muscarinic M1 receptors. It is also a highly competitive antagonist at cardiac M2 receptors and ileal M3 muscarinic receptors.

1-Carboxycyclohexaneacetic acid may be present as a potential impurity in commercial gabapentin, an antiepileptic drug. Furthermore, it serves as a precursor for synthesizing antagonists targeting the serotonin (5-HT) receptor subtype 5-HT2A.

13,14-dihydro-15-keto Prostaglandin E2 (13,14-dihydro-15-keto PGE2) serves as the predominant metabolite of PGE2 in plasma, created through a 15-keto PGE2 intermediate by the action of 15-oxo-PG Δ13 reductase. Unlike its precursor PGE2, this compound exhibits poor binding affinity towards EP2 and EP4 PGE2 receptors (Ki values of 12 and 57 µM, respectively) in CHO cells and fails to stimulate adenylate cyclase activity therein (EC50s >18 and >38 µM, respectively). Concentrations of 13,14-dihydro-15-keto PGE2 are notably higher in the plasma of pregnant women during their third trimester and at labor and delivery stages, whereas its levels are found to be reduced in the tumor tissues of patients with non-small cell lung cancer (NSCLC) compared to adjacent healthy tissue.

Compound 24 (5-HT2 agonist-1 free base) is a potent agonist for 5-HT2A, 5-HT2B, and 5-HT2C receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM,

5-HT2C agonist-3 ((+)-19) free base, a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), exhibits antipsychotic drug-like activity and inhibits Amphetamine-

Brilaroxazine (RP5063): multimodal dopamine/5-HT modulator, partial agonist at D2/D3/D4, 5-HT1A/2A, and antagonist at 5-HT2B/7.

MDL-74156 is an active metabolite of dolasetron and a 5-hydroxy-tryptamine3 (5-HT3) antagonist.

Butriptyline (Butriptylene), a tricyclic antidepressant, is effective when administered orally [1].

GABA-IN-2 (Compound 5), a GABA inhibitor, exhibits both larvicidal and insecticidal properties, achieving an 87% mortality rate at a concentration of 50 mg/L [1

TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).