Neurokinin B belongs to the tachykinin family of peptides. Neurokinin B binds a family of GPCRs—including neurokinin receptor 1 (NK1R), NK2R, and NK3R-to mediate their biological effect.
Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3].
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis[1]. CME: Clathrin mediated endocytosis
Uldazepam is a benzodiazepine derivative and can be used to treat patients with anxiety syndromes as tranquilizer.
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5[1].
MS012 is a potent and selective inhibitor of G9a-Like Protein (GLP) lysine methyltransferase with IC50 of 7 nM, shows >30-fold selectivity for GLP over G9a and other methyltransferases.
D-Pentamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Pentamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.
Synephrine (Oxedrine) hemitartrate, an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine hemitartrate is a sympathomimetic compound and can be used for weight loss[1][2].
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research[1][2].
L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake[1][2][3].
Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.Target: mAChROxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination (urge incontinence), by decreasing muscle spasms of the bladder. Oxybutynin competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor. It also has direct spasmolytic effects on bladder smooth muscle as a calcium antagonist and local anesthetic, but at concentrations far above those used clinically. Oxybutynin is available orally in generic formulation or as the brand-names Ditropan, Lyrinel XL, or Ditrospam, as a transdermal patch under the brand name Oxytrol, and as a topical gel under the brand name Gelnique. Oxybutynin is also a possible treatment of hyperhidrosis (hyper-active sweating) [1-3].
XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.IC50 value: 3 nMTarget: NaV1.7in vitro: XEN907 shows a further 10-fold increase in potency, represents a promising structure for further optimization efforts. XEN907 shows no significant activity at 10 μM against a broad panel of 63 receptors and transporters. Determination of the ADME properties of XEN907 reveals that XEN907 is not cytotoxic and has favourable hepatocyte metabolic stability for both human and dog, although inhibition of CYP3A4 is observed in a recombinant human enzyme assay.[1]in vivo: Pharmacokinetic analysis in rats of XEN907 demonstrates that, consistent with the compound's ADME parameters, the compound is modestly bioavailable. Following an initial rapid absorption phase (oral Tmax = 20 min), XEN907 is extensively distributed (Vss 600-fold higher than the plasma volume in rats) and rapidly cleared. [1]
Pilocarpine is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Brasofensine (BMS-204756) sulfate is a dopamine transporter antagonist and can be used for parkinson’s disease research[1].
gamma-DGG is a competitive AMPA receptor blocker.
Tenuifoliside B, a component isolated from Polygalae Radix, inhibits potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment. Tenuifoliside B shows potential cognitive improvement and cerebral protective effects. Tenuifoliside B has potential to become an anti-AD lead compound[1][2].
Acetyl-Tau Peptide (273-284) amide is an acetylated Tau peptide fragment. Acetyl-Tau Peptide (273-284) amide limits the substantial aggregation of Ac-Aβ(25–35)-NH2 and can be used as an inhibitor of Ac-Aβ(25–35)-NH2. Acetyl-Tau Peptide (273-284) amide can be used as an experimental model to investigate the Aβ/Tau cross-interaction [1][2].
Aβ42 agonist-1 (compound 7a) is a small molecule compound that can promote Aβ42 aggregation. Aβ42 agonist-1 can interact with Aβ42 oligomers and pentamers to promote nontoxic aggregate self-assembly and rapid fibril formation. Aβ42 agonist-1 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells[1].
Epiberberine chloride, a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
Small cardioactive peptide A (SCPA) is a neuropeptide that can be obtained from Aplysia[1].
7,8-Dihydroneopterin, an inflammation marker, induces cellular apoptosis in astrocytes and neurons via enhancement of nitric oxide synthase (iNOS) expression. 7,8-Dihydroneopterin can be used in the research of neurodegenerative diseases[1].
Bavisant Hcl (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
6-Methoxykaempferol 3-O-Rutinoside is a natural product isolated from the herbs of Pilocarpus pennatifolius[1].
Galanin (1-19), human is the 1-19 fragment of the human galanin. Galanin (GAL) is a widely distributed neuropeptide with diverse biological effectsincluding modulation of hormone release, antinociception and modification of feeding behavior[1].
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
Glycine-13C2 is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
TMB-8 is a novel Ca 2+ antagonist. TMB-8 may exert inhibitory effects in smooth muscle by blocking Ca 2+ release from intracellular bound stores.