Sinomenine hydrochloride is a blocker of the NF-κB activation and also an activator of μ-opioid receptor.
Iloperidone (hydrochloride) is a D(2)/5-HT(2) receptor antagonistis, which is an atypical antipsychotic for the treatment of schizophrenia symptoms.Target: 5-HT receptor; Dopamine receptorIloperidone (hydrochloride) is the hydrochloride of iloperidone, iloperidone (HP 873; 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy] -3- methoxyphenyl]ethanone) is a compound currently in clinical trials for the treatment of schizophrenia. Iloperidone displays affinity for dopamine D2 receptors and for 5-HT2A receptors and has a variety of in vivo activities suggestive of an atypical antipsychotic. Iloperidone displayed higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displayed high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively), and was found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM) [1]. Iloperidone was eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events [2]. Iloperidone pharmacokinetics and pharmacodynamics are presented herein, together with an evaluation of clinical safety and efficacy results [3].Clinical indications: Post traumatic stress disorder; Schizophrenia Toxicity: Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased.
Eprobemide is a non-competitive reversible inhibitor of monoamine oxidase A.
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response[1][2].
Irindalone is a novel serotonin 5-HT2 antagonist.
Loperamide hydrochloride is an opiate receptor agonist for the treatment of diarrhea.
Oxiperomide is an orally active dopamine-blocking agent[1].
GYKI 52466 is a potent antagonist of kainate- and AMPA-activated currents (IC50 values, 7.5 and 11 μM, respectively), GYKI 52466 can be used for the research of neurological disorders, such as Parkinson's disease[1].
Fenitrothion-d6 is the deuterium labeled Fenitrothion[1]. Fenitrothion, one of the most widely used organophosphorus pesticides, is a cholinesterase inhibiting insecticide/acaricid. Fenitrothion is widely used, as a broad-spectrum insecticide, on cotton crops, vegetables crops, fruit crops, and field crops especially paddy. Fenitrothion leads to accumulation of nitrophenols[2][3].
Milnacipran-d10 hydrochloride is the deuterium labeled Milnacipran hydrochloride. Milnacipran hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia[1][2].
Autocamtide 2 is a highly selective peptide substrate of calcium/calmodulin-dependent protein kinase II (CaMKII). It can be used in the CaMKII activity assay.
Alpidem selectively binds to α1β2γ2 subunit-containing GABAA receptor with an IC50 of 17 nM and exerts anxiolytic effect[1].
Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC50 of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder[1].
GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant[1].
PMPA (NMDA antagonist) is an NMDA receptor antagonist with Ki values of 0.84, 2.74, 3.53 and 4.16 μM for NR2A, NR2B, NR2C and NR2D, respectively[1].
BDZ-g is a potent, selective antagonist of AMPA receptor. BDZ-g has the potential for the research of various neurological disorders involving excessive activity of AMPA receptors[1].
Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice[1][2].
Tertatolol is a potent antagonist of beta-adrenoceptor and 5-HT receptor, with unique renal vasodilatatory effects.
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile[1].
DL-AP7 is a competitive NMDA antagonist and an anticonvulsant. DL-AP7 blocks the NMDA-induced convulsions and impairs learning performance in a passive avoidance task in mice[1].
DL-AP5 is a NMDA (N-methyl-D-aspartate) receptor antagonist. DL-AP5 shows significantly antinociceptive activity. DL-AP5 specifically blocks on channels in the rabbit retina[1][2].
L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action[1][2].
3-Hydroxy agomelatine D3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM[1].
BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC50 of 56 nM[1].
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis. NGB 2904 hydrochloride can inhibit Cocaine's rewarding effects and Cocaine-induced reinstatement of drug-seeking behavior[1][2].
Prucalopride-13C,d3 is the 13C- and deuterium labeled.
MAO-IN-3 (Compound 5) is a reversible and competitive MAO inhibitor (Ki: 0.6 and 0.2 μM for MAO A and MAO B). MAO-IN-3 inhibits LN-229 glioblastoma cell proliferation with an IC50 of 0.8 μM. MAO-IN-3 can be used for cancer research[1].
β-Lipotropin (60-65) (β-LPH (60-65)), an opioid peptide, is a potent opioid agonist[1].
Amitriptylinoxide (Equilibrin) is an analogue and metabolite of amitriptyline with similar antidepressant efficacy[1].