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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Apoptosis >
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Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
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NF-κB >
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Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
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Tetrahydroberberine

Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).

  • CAS Number: 522-97-4
  • MF: C20H21NO4
  • MW: 339.385
  • Catalog: Dopamine Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 476.1±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 141.1±25.9 °C

FK1052 hydrochloride

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.

  • CAS Number: 129299-81-6
  • MF: C18H20ClN3O
  • MW: 329.824
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(D-Ala4)-Substance P (4-11)

[DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes[1].

  • CAS Number: 81381-50-2
  • MF: C44H65N11O10S
  • MW: 940.120
  • Catalog: Neurokinin Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1450.5±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 831.0±34.3 °C

Cogentin

Benztropine mesylate is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research[1]. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2].

  • CAS Number: 86-13-5
  • MF: C21H25NO
  • MW: 307.42900
  • Catalog: Dopamine Receptor
  • Density: 1.11g/cm3
  • Boiling Point: 409ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 120.1ºC

CGP 7930

CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons[1].

  • CAS Number: 57717-80-3
  • MF: C19H32O2
  • MW: 292.45600
  • Catalog: GABA Receptor
  • Density: 0.971g/cm3
  • Boiling Point: 364.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 152.6ºC

L-2-AMINO-4-SULFOBUTYRIC ACID

L-Homocysteic acid (L-HCA) is an endogenous excitatory amino acid that acts as a NMDA receptor agonist (EC50: 14 μM). L-Homocysteic acid is neurotoxic, and can be used in the research of neurological disorders[1][2][3].

  • CAS Number: 14857-77-3
  • MF: C4H9NO5S
  • MW: 183.18300
  • Catalog: iGluR
  • Density: 1.638g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-3084014

Nirogacestat (PF-3084014) is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.

  • CAS Number: 1290543-63-3
  • MF: C27H41F2N5O
  • MW: 489.64400
  • Catalog: γ-secretase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

U-89843A

U-89843A is an allosteric modulator of GABAA receptor. U-89843A enhances GABA-induced Cl- currents[1].

  • CAS Number: 157013-85-9
  • MF: C16H24ClN5
  • MW: 321.85
  • Catalog: GABA Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nitenpyram

Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals[1][2].

  • CAS Number: 150824-47-8
  • MF: C11H15ClN4O2
  • MW: 270.715
  • Catalog: nAChR
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 417.2±45.0 °C at 760 mmHg
  • Melting Point: 72ºC
  • Flash Point: 206.1±28.7 °C

Roxindole hydrochloride

Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities[1][2][3].

  • CAS Number: 108050-82-4
  • MF: C23H27ClN2O
  • MW: 382.92600
  • Catalog: Dopamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Salsolidine hydrochloride

Salsolidine hydrochloride, a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A (monoamine oxidase A) inhibitor.

  • CAS Number: 63283-42-1
  • MF: C12H18ClNO2
  • MW: 243.73
  • Catalog: Monoamine Oxidase
  • Density: N/A
  • Boiling Point: 313.4ºC at 760 mmHg
  • Melting Point: 189-192ºC
  • Flash Point: 127.1ºC

L-Glutamic acid-13C2

L-Glutamic acid-13C2 is the 13C labeled L-Glutamic acid[1]. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals[2].

  • CAS Number: 115473-56-8
  • MF: C313C2H9NO4
  • MW: 149.11
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

α-Conotoxin GIC

α-Conotoxin GIC is a potent and selective α3β2 nicotinic antagonist with an IC50 of 1.1 nM[1].

  • CAS Number: 757236-92-3
  • MF: C61H92N24O20S4
  • MW: 1609.79
  • Catalog: nAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Arg-Glu(EDANS)-(Asn670,Leu671)-Amyloid β/A4 Protein Precursor770 (668-675)-Lys(DABCYL)-Arg trifluoroacetate salt

RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide,serves as a fluorescent substrate for BACE1(Em=360nm,Ex=528nm). RE (EDANS) EVNLDAEFK (DABCYL) R can be used for BACE1 activity measurement and the enzyme activity level is directly proportional to the fluorescence reaction[1].

  • CAS Number: 310427-94-2
  • MF: C91H129N25O25S
  • MW: 2005.22
  • Catalog: Beta-secretase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GP3269

GP3269 is a potent, selective, and orally active inhibitor of human adenosine kinase (AK) with an IC50 of 11 nM. GP3269 exhibits anticonvulsant activity in rats[1].

  • CAS Number: 186393-42-0
  • MF: C23H21FN4O3
  • MW: 420.44
  • Catalog: Adenosine Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Neboglamine hydrochloride

Neboglamine (CR-2249, XY-2401) hydrochloride is an orally active NMDA receptor glycine site positive modulator that can be used in schizophrenia research[1].

  • CAS Number: 2759182-59-5
  • MF: C13H25ClN2O3
  • MW: 292.80
  • Catalog: iGluR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tiotropium-d6 bromide

Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.

  • CAS Number: 1126775-44-7
  • MF: C19H16D6BrNO4S2
  • MW: 478.45
  • Catalog: mAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ansofaxine hydrochloride

Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.

  • CAS Number: 916918-84-8
  • MF: C24H32ClNO3
  • MW: 417.97
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UNC9995

UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions[1].

  • CAS Number: 1354030-52-6
  • MF: C20H21Cl2N3OS
  • MW: 422.37
  • Catalog: Dopamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Blonanserin dihydrochloride

Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension[1][2].

  • CAS Number: 132812-45-4
  • MF: C23H32Cl2FN3
  • MW: 440.42
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-HT2 agonist-1 free base

5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].

  • CAS Number: 2708279-77-8
  • MF: C19H22N2O2
  • MW: 310.39
  • Catalog: 5-HT Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Alizapride

Alizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders[1][3].

  • CAS Number: 59338-93-1
  • MF: C16H21N5O2
  • MW: 315.37000
  • Catalog: Dopamine Receptor
  • Density: 1.224 g/cm3
  • Boiling Point: 597.6ºC at 760 mmHg
  • Melting Point: 3360°C
  • Flash Point: 315.2ºC

Flumazenil

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

  • CAS Number: 78755-81-4
  • MF: C15H14FN3O3
  • MW: 303.288
  • Catalog: GABA Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 528.0±50.0 °C at 760 mmHg
  • Melting Point: 201-203°C
  • Flash Point: 273.1±30.1 °C

BMS-986121

BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs[1][2][3].

  • CAS Number: 313671-26-0
  • MF: C15H9Cl2N3O2S
  • MW: 366.22
  • Catalog: Opioid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY-411575 (isomer 1)

LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

  • CAS Number: 209984-58-7
  • MF: C26H23F2N3O4
  • MW: 479.47500
  • Catalog: γ-secretase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH 125

NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also could induce eEF2 phosphorylation, with an IC50 of 60 nM for eEF-2K.

  • CAS Number: 278603-08-0
  • MF: C27H45IN2
  • MW: 524.564
  • Catalog: CaMK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 88.2-94.9ºC
  • Flash Point: N/A

(±)-Marmesin

(±)-Marmesin is a good precursor of the linear furanocoumarins. (±)-Marmesin derivatives have high degree of acetylcholinesterase inhibitory property[1][2].

  • CAS Number: 13710-70-8
  • MF: C14H14O4
  • MW: 246.259
  • Catalog: AChE
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 434.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 168.0±22.2 °C

ABT 894

Sofiniclin (ABT 894) is an agonist of nicotinic acetylcholine receptor (nAChR), used as a potential non-stimulant treatment for attention-deficit/hyperactivity disorder (ADHD).

  • CAS Number: 799279-80-4
  • MF: C10H11Cl2N3
  • MW: 244.12000
  • Catalog: nAChR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DWK-1339

DWK-1339 is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.

  • CAS Number: 1018946-38-7
  • MF: C20H22O4
  • MW: 326.38600
  • Catalog: Amyloid-β
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Naxagolide

Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD)[1][2].

  • CAS Number: 88058-88-2
  • MF: C15H21NO2
  • MW: 247.333
  • Catalog: Dopamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 391.7±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 190.7±27.9 °C