Neuronal Signaling is involved in the regulation of the mechanics of the central nervous system such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells).

G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, and etc, are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. GPCRs are activated by diverse stimuli, including light, enzymatic processing of their N-termini, and binding of proteins, peptides, or small molecules such as neurotransmitters, and regulate neuronal excitability by indirectly modulating the function of voltage-gated channels, such as voltage-gated calcium channel and transient receptor potential (TRP) ion channels. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation.

GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

References:
[1] Lathia JD, et al. J Neurochem. 2008 Dec;107(6):1471-81.
[2] Palczewski K, et al. Annu Rev Neurosci. 2013 Jul 8;36:139-64.
[3] Geppetti P, et al. Neuron. 2015 Nov 18;88(4):635-49.


Anti-infection >
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MK-7622

MK-7622 is a muscarinic M1 receptor positive allosteric modulator.Target: M1 receptorMK-7622 is useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders.

  • CAS Number: 1227923-29-6
  • MF: C25H25N3O2
  • MW: 399.485
  • Catalog: mAChR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 643.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 342.7±34.3 °C

AM-6494

AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM)[1].

  • CAS Number: 1874232-80-0
  • MF: C22H21F2N5O3S
  • MW: 473.50
  • Catalog: Beta-secretase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Quinpirole dihydrochloride

rel-Quinpirole (rel-LY 141865) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases[1].

  • CAS Number: 73625-62-4
  • MF: C13H22ClN3
  • MW: 255.78700
  • Catalog: Dopamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB-277011

SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.IC50 value: 8.0 (pKi)Target: D3 receptor

  • CAS Number: 215803-78-4
  • MF: C28H30N4O
  • MW: 438.564
  • Catalog: Dopamine Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 679.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 364.6±31.5 °C

NMDA receptor modulator 4

NMDA receptor modulator 4 (Compound 169) is a potent NMDA receptor modulator. NMDA receptor modulator 4 can be used for neurological disorder research[1].

  • CAS Number: 2758256-71-0
  • MF: C13H9F3N2O3S
  • MW: 330.28
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chrysin 6-C-glucoside 8-C-arabinoside

Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research[1].

  • CAS Number: 185145-34-0
  • MF: C26H28O13
  • MW: 548.49
  • Catalog: CGRP Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(±)-Darifenacin

(±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].

  • CAS Number: 133033-93-9
  • MF: C28H30N2O2
  • MW: 426.55
  • Catalog: mAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ziprasidone mesylate

Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].

  • CAS Number: 185021-64-1
  • MF: C22H25ClN4O4S2
  • MW: 509.04
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK1521498

GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs[1].

  • CAS Number: 1426543-84-1
  • MF: C24H23F2N4O4P
  • MW: 500.43
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ro 41-0960

Ro 41-0960 is a selective catechol-O-methyltransferase(COMT) inhibitor[1].

  • CAS Number: 125628-97-9
  • MF: C13H8FNO5
  • MW: 277.20500
  • Catalog: COMT
  • Density: 1.536g/cm3
  • Boiling Point: 489.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 250.1ºC

(S)-WAY 100135

(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of 5-HT 1A (IC50=33.9 nM). (S)-WAY 100135 dihydrochloride has anxiolytic activity in animal models[1].

  • CAS Number: 149007-54-5
  • MF: C24H35Cl2N3O2
  • MW: 468.46
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MPDC

MPDC is a potent and competitive inhibitor of the Na+-dependent high-affinity glutamate transporter in forebrain synaptosomes[1].

  • CAS Number: 159262-32-5
  • MF: C7H9NO4
  • MW: 171.15
  • Catalog: GlyT
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 381.2±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 184.4±27.9 °C

Usmarapride

Usmarapride (SUVN-D4010) is a selective 5-HT4 receptor ligand with EC50 value 27.5nM, intended for the symptomatic research of Alzheimer's disease and other disorders of memory and cognition like attention deficient hyperactivity, Parkinson's and schizophrenia[1].

  • CAS Number: 1428862-33-2
  • MF: C23H31N5O6
  • MW: 473.52
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AChE-IN-31

AChE-IN-31 (compound 1) is a non-competitive AChE inhibitor with potential for the study of Alzheimer's disease[1].

  • CAS Number: 1325209-07-1
  • MF: C27H44Na2O9S2
  • MW: 622.74
  • Catalog: AChE
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ro 25-6981 hydrochloride

Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD)[1][2][3].

  • CAS Number: 919289-58-0
  • MF: C22H30ClNO2
  • MW: 375.93
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CR4056

CR4056 is a selective inhibitor of human recombinant MAO-A with an IC50 of 202.7 nM. CR4056 is also a ligand of imidazoline-2 receptor (I2R) with an IC50 of 596 nM.

  • CAS Number: 1004997-71-0
  • MF: C17H12N4
  • MW: 272.304
  • Catalog: Imidazoline Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 364.1±24.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 174.0±22.9 °C

Usmarapride free base

Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease[1].

  • CAS Number: 1428862-32-1
  • MF: C21H29N5O2
  • MW: 383.487
  • Catalog: 5-HT Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 541.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 281.5±32.9 °C

Serotonin-d4

Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.

  • CAS Number: 58264-95-2
  • MF: C10H8D4N2O
  • MW: 180.24
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TIK-301

TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment[1][2][3].

  • CAS Number: 118702-11-7
  • MF: C14H17ClN2O2
  • MW: 280.750
  • Catalog: 5-HT Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 525.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 271.9±30.1 °C

U-69593

U-69593 is a potent and selective κ1-opioid receptor agonist[1]. U-69593 attenuates cocaine-induced behavioral sensitization in the rat[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum[4].

  • CAS Number: 96744-75-1
  • MF: C22H32N2O2
  • MW: 356.50
  • Catalog: Opioid Receptor
  • Density: 1.14g/cm3
  • Boiling Point: 518.719ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 267.512ºC

Vomifoliol

Vomifoliol, a compound related to abscisie acid (ABA), has a modified 2,4-pentadiene side chain and has activity equal to that displayed by ABA. Vomifoliol exhibits antiacetylcholinesterase activity and displays moderate antileishmanial activity[1][2].

  • CAS Number: 23526-45-6
  • MF: C13H20O3
  • MW: 224.296
  • Catalog: AChE
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 362.3±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 187.1±24.4 °C

Moclobemide N-Oxide

Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitory activity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm[1][2].

  • CAS Number: 64544-24-7
  • MF: C13H17ClN2O3
  • MW: 284.74
  • Catalog: Monoamine Oxidase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amyloid β-Protein (1-11)

β-amyloid (1-11) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.

  • CAS Number: 190436-05-6
  • MF: C56H76N16O22
  • MW: 1325.3
  • Catalog: Peptides
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-methylcytisine

N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia[1][2].

  • CAS Number: 486-86-2
  • MF: C12H16N2O
  • MW: 204.27
  • Catalog: nAChR
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 400.8±34.0 °C at 760 mmHg
  • Melting Point: 137-139ºC
  • Flash Point: 191.9±18.0 °C

Rasagiline 13C3 (mesylate racemic)

Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible inhibitor of monoamine oxidase.

  • CAS Number: 1216757-55-9
  • MF: C10(13C)3H17NO3S
  • MW: 270.32
  • Catalog: Monoamine Oxidase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SSR 180711 hydrochloride

SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus[1].

  • CAS Number: 446031-79-4
  • MF: C14H18BrClN2O2
  • MW: 361.66
  • Catalog: nAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oxetorone

Oxetorone fumarate is a non-selective, orally active serotonin antagonist. Oxetorone fumarate is an antimigraine agent[1].

  • CAS Number: 34522-46-8
  • MF: C25H25NO6
  • MW: 435.46900
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-[(2S)-2-Aminopropyl]-1H-indazol-6-ol

AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent[1][2].

  • CAS Number: 210580-75-9
  • MF: C10H13N3O
  • MW: 191.23
  • Catalog: 5-HT Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 372.8±22.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 179.2±22.3 °C

Z1078601926

Z1078601926 is an allosterical inhibitor of human dopamine transporter (hDAT). Z1078601926 has synergistic effect with Nomifensine (HY-B1110)[1].

  • CAS Number: 1493256-85-1
  • MF: C14H19FN2O
  • MW: 250.31
  • Catalog: Dopamine Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

broflanilide

Broflanilide is a potential insecticide and metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM.

  • CAS Number: 1207727-04-5
  • MF: C25H14BrF11N2O2
  • MW: 663.277
  • Catalog: GABA Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 467.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 236.8±28.7 °C