Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].
AnnH31 is a potent Inhibitor of DYRK1A Kinase.
PACAP (1-38), human, ovine, rat is a neuropeptide with 38 amino acid residues. PACAP (1-38) binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively.
Geissoschizoline ((+)-Geissoschizoline) is a potent inhibitor of human AChE/BChE, with IC50s of 20.40 µM and 10.21 µM, respectively. Geissoschizoline emerges as a possible multi-target prototype that can be very useful in studies of preventing neurodegeneration and restoring neurotransmission. Geissoschizoline aiso is a potent anti-inflammatory agent[1].
Medifoxamine is a monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake[1].
Mrgx2 antagonist-2 is a Mrgx2 antagonist (Example 123 in reference patent) with a pIC50 of 8.6. Mrgx2 antagonist-2 can be used in the research of MrgX2 -mediated diseases or disorders[1].
A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.IC50 value: 1.6 nM(EC50) [1]Target: CB2 agonistin vitro: In radioligand binding assays, A-836339 displays high affinities at CB(2) receptors and selectivity over CB(1) receptors in both human and rat.In addition A-836339 exhibits a profile devoid of significant affinity at other G-protein-coupled receptors and ion channels [1].in vivo: In the complete Freund's adjuvant model of inflammatory pain, A-836339 exhibits a potent CB(2) receptor-mediated antihyperalgesic effect that is independent of CB(1) or mu-opioid receptors. A-836339 has also demonstrated efficacies in the chronic constrain injury (CCI) model of neuropathic pain, skin incision, and capsaicin-induced secondary mechanical hyperalgesia models [1]. Similar to systemic delivery, intra-spinal injection of A-836339 (0.3 and 1 nmol) also attenuated both von Frey-evoked and spontaneous firing of WDR neurons in neuropathic rats. Intra-spinal injections of A-836339 were ineffective in sham rats [2]. Systemic A-836339 and AM1241 produced dose-dependent efficacy in both inflammatory and neuropathic pain models. Local administration of CB? agonists also produced significant analgesic effects in SNL (intra-DRG and i.t.) and CFA (intra-DRG) pain models [3].
BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65) specific agonist. BTB09089 increases TDAG8 expression and regulates the cytokine production of T cells and macrophages[1].
MAO-B-IN-27 (Compound 12c) is a monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-27 has potent and selective MAO-B inhibitory effect for hMAO-B with an IC50 values of 8.9 nM. MAO-B-IN-27 can be used for the research of parkinson's disease (PD)[1].
RU 23686 free base is a piperidinylindole derivative. RU 23686 free base can be used to investigate the extent to which different neurotransmitters by the interaction with pharmacological agents[1].
4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1][2].
CGP 36742 is a selective GABAB receptor antagonist that can penetrate the blood–brain barrier after peripheral administration, with an IC50 of 32 μM. CGP 36742 is useful in treatment of depression[1].
Eletriptan-d3 (Eletriptan-d3 HBr) is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
AChE/BChE-IN-11 (compound 1) is a potent is a dual AChE and BChE inhibitor with IC50 values of 70 and 71 μM for AChE and BChE, respectively. AChE/BChE-IN-11 is a natural product that could be isolated from the leaf of artichoke . AChE/BChE-IN-11 can be used in research of Alzheimer’s disease (AD) research[1].
AChE-IN-19 (compound A15) is a highly potent AChE inhibitor with an IC50 value of 0.56 μM, also inhibits Aβ aggregation. AChE-IN-19 has potent neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE-IN-19 can be used for researching Alzheimer's disease[1].
XJB-5-131 is a mitochondria-targeted ROS and electron scavenger[1]. XJB-5-131 is a bi-functional antioxidant that comprises a radical scavenger. XJB-5-131 is a synthetic antioxidant that targets mitochondria[2]. XJB-5-131 is an effective ionizing irradiation protector and mitigator of cord blood mononuclear cells (CB MNCs)[3].
Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system[1]..
Desmethylnortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1].
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.Target: 5- HT3 ReceptorIC50 Value: in vitro: 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) [1]. The 5-HT3A receptor antagonist ondansetron (0.3 nM) reversibly inhibited the 5-HT (30 microM) signal by 70% and at 3 nM it abolished the response [2].in vivo: Acute ondansetron administration at the lowest dose (0.1 mg/kg, IP) tested had no effect, while other doses (0.33 and 1 mg/kg, IP) produced improvements in auditory gating [3]. Different doses of ondansetron were injected intraperitoneally (i.p.) at fixed times during the day to determine both the sublethal (TD50) and lethal (LD50) doses, which were, respectively, 3.7 +/- 0.6 mg/kg and 4.6 +/- 0.5 mg/kg [4]. ondansetron (0.25-1.0 mg/kg, subcutaneously) given before the challenge dose of ethanol (2.4 g/kg, intraperitoneally) injection, significantly and dose dependently attenuated the expression of sensitization. In addition, ondansetron (1.0 mg/kg, subcutaneously) given before ethanol injection on days 1, 4, 7, and 10 significantly blocked the development (days 1, 4, 7, and 10), and expression (day 15) of sensitization to the locomotor stimulant effect of ethanol injection [5]. Toxicity: Ondansetron may be safe in lower doses used to prevent nausea and vomiting in radiation treatment or postoperatively. However, as there is a report that a lower dose of ondansetron prolonged the QT interval in healthy volunteers, this needs to be clarified by the FDA [6].
Hydroquinidine is an antiarrhythmic agent.
A new tertiary amine, Oxyphencyclimine hydrochloride，has been investigated for its effects on the peripheral parasympathetic system. was essentially the most potent in depressing gastric secretion.
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment[1][2].
(Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively[1].
PF-00217830 is a serotonin 1A receptor agonist, dopamine D2 receptor agonist, and serotonin 2A receptor antagonist.PF-00217830 may be used in the study of schizophrenia.
IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders[1].
Tetrabenazine is a VMAT-inhibitor used for treatment of hyperkinetic movement disorder.Target: Otherstetrabenazine (TBZ), a monoamine-depleting and a dopamine-receptor-blocking drug. TBZ is an effective and safe drug for the treatment of a variety of hyperkinetic movement disorders. In contrast to typical neuroleptics, TBZ has not been demonstrated to cause tardive dyskinesia [1, 2]. Twenty patients with tardive dyskinesia (mean duration = 43.7 months) were videotaped before and after tetrabenazine treatment. One patient did not tolerate tetrabenazine owing to sedation. The remaining 19 were rated after a mean of 20.3 weeks at a mean tetrabenazine dose of 57.9 mg/day. There were significant improvements in mean scores on both the patient AIMS self-rating and the AIMS motor subset evaluated by the blind videotape raters. All 19 patients continued to take tetrabenazine after the study [3].
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O[1][2].
Nardoguaianone J, a guaiane-type compound, can be isolated from Nardostachys chinensis roots. Nardoguaianone J can enhance SERT activity[1][2].
Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.