Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders[1].
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist[1].
EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects[1].
FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.
Tasimelteon is a melatonin MT1 and MT2 receptor agonist.Target: melatonin receptorTasimelteon is a novel circadian regulator, is the first product for the treatment of Non-24-hour Sleep-Wake Disorder (Non-24) approved by either the FDA or the European Medicines Agency (EMA). Tasimelteon is a potent and specific melatonin (MT1 and MT2) receptor agonist with 2 - 4 times greater affinity for the MT2 receptor.
Bodipy TMR-X muscimol is a Bodipy labeled Muscimol (HY-N2313) (Ex=543 nm, Em=572 nm). Muscimol is a GABAA agonist. Bodipy TMR-X muscimol can be used for imaging the spread of reversible brain inactivations[1].
LY 392098 is a selective, potent and centrally active positive allosteric modulator of AMPAR; enhances glutamate (100 uM) stimulated ion influx through recombinant homomeric human AMPAR ion channels with EC50 of 1.77 uM (GluR1(i)), 0.22 uM (GluR2(i)), 0.56 uM (GluR2(o)), 1.89 uM (GluR3(i)) and 0.20 uM (GluR4(i); enhances a dose-dependent manner responses to AMPA, potentiates the synaptic excitation of dentate granule cells following perforant path stimulation in vivo.
BAM-22P, a highly potent opioid peptide, is a potent opioid agonist.
Metofenazate is a selective calmodulin inhibitor.
Fluphenazine decanoate dihydrochloride is a dopamine D2 receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research[1][2][3].
TAK-071 is a novel muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM[1].
Calmidazolium chloride (R 24571) is a calmodulin (CaMK) antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively[1]. Also in anti-cancer research[2]. Calmidazolium binds to CaMK with a Kd of 3 nM.
Corynoline, isolated from Corydalis incise (Papaveraceae), is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM[1]. Corynoline exhibits anti-inflammatory activity by activating Nrf2[2].
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
Decanoic acid-d19 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity)[1][2][3][4].
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.IC50 value: 4.6 nM [1]Target: FAAH in vitro: URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH [1]. URB597 reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide [2]. in vivo: URB597 inhibits [3H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. URB597 enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH [3]. When delivered intraperitonealy (0.3 mg/kg) URB597 reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain [4].
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][5][6].
ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC50 of 120 nM and an EC50 of 129 nM, respectively[1].
AChE-IN-44 (Compound Tap4) is an AChE inhibitor. AChE-IN-44 can be converted into the thiazole salt AChE inhibitor Tat2[1].
7-Chlorokynurenic acid sodium salt is a selective antagonist at the glycine modulatory site of the N-methyl-D-aspartate receptor complex and also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM.
l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease[1][2][3].
Doxacurium chloride (BW A938U) is a potent non-depolarizing neuromuscular blocking agent. Doxacurium chloride binds to cholinergic receptors to antagonize acetylcholine, resulting in a block of neuromuscular transmission. Doxacurium chloride can be used for the research of neurological diseases[1].
KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). IC50 value:Target: KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning[1].
Cyclobenzaprine Hcl is a skeletal muscle relaxant and a central nervous system (CNS) depressant.Target: 5-HT Receptor 2ACyclobenzaprine is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine was thought to be an alpha 2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. Cyclobenzaprine reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the alpha 2-adrenoceptor antagonists idazoxan and yohimbine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by 6-hydroxydopamine. Cyclobenzaprine is a 5-HT2 receptor antagonist and that its muscle relaxant effect is due to inhibition of serotonergic, not noradrenergic, descending systems in the spinal cord [1]. The inhibitory effects of cyclobenzaprine on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT(2) receptors in the spinal cord [2].
Ethaverine hydrochloride, a derivative of papaverine, inhibits cardiac L-type calcium channel. Ethaverine hydrochloride is a peripheral vasodilator and antispasmodic agent. Ethaverine hydrochloride can be used for research of peripheral vascular disease[1][2][3].
Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD)[1].