Azacosterol (Diazasterol) is a DHCR24 inhibitor.Azacosterol undergoes a series of reactions in cortical neurons following oral or intraperitoneal administration.

Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

Teriparatide acetate (Forteo) is a PHT agonist, with an IC50 of 2 nM in HEK293 cells.Teriparatide acetate is a recombinant form of parathyroid hormone. It is an effective anabolic (i.e., bone growing) agent used to treat some forms of osteoporosis. Intermittent use of Teriparatide acetate activates osteoblasts more than osteoclasts, which leads to an overall increase in bone.

Apamin acetate (Apamine acetate) is a selective Ca2+-activated blocker of K+ (SK) channels, an 18-amino acid peptide neurotoxin found in bee toxins.Apamin acetate enhances synapse growth and regeneration following laceration injury to cortical neurons.Apamin acetate has anti-inflammatory and anti-fibrotic effects.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. It binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate is a highly potent antagonist of parathyroid hormone (PTH) The Ki value is 69 nM in bovine renal cortical membrane.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

Neuropeptide Y (29-64), amide, human acetate is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.

Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.

SR 57227 hydrochloride(SR 57227A ) is a potent, orally active and selective 5-HT3 receptor agonist. It with ability to cross the blood brain barrier. It has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs/cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in mice. This compound holds potential for osteoporosis research [1] [2].

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

Paeonilactone B ((+)-Paeonilactone B), a monoterpenoid from Paeonilactone, has neuroprotective activity, inhibits oxidative stress, and suppresses H2O2-induced neurotoxicity in rat cortical cells.

Pirepemat (IRL752) is a cortical-preferring catecholamine agent that enhances cognition. It is utilized in the investigation of Parkinson's disease.

Flufenazine is an antipsychotic drug. It is used to treat chronic mental illnesses such as schizophrenia. Flufenazine works by blocking postsynaptic dopamine D2 receptors in the limbic system, cortical system, and basal ganglia. This prevents the effects

GluN2B (formally NR2B) selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC50 = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing GluN2B (formally NR2B), but not GluN2A (formally

Paeonilactone C significantly protects primary cultures of rat cortical cells against H2O2-induced neurotoxicity.

Talipexole dihydrochloride (Domnin) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist, and 5-HT3 receptor antagonist in both rat cortical and intestinal membrane fractions with Ki values of 0.35 μM and 0.22 μM, respectively. It displays antiParkinsonian activity.

CP 465022 hydrochloride is a potent, and selective noncompetitive antagonist of AMPA receptor with anticonvulsant activity. CP 465022 hydrochloride inhibits Kainate-induced response with an IC50 of 25 nM in rat cortical neurons.

(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in the renal cortical collecting duct when used at a concentration of 100 nM.[5]11(12)-EET (50 μg/kg per day) increases adhesion of isolated peripheral blood leukocytes in a chamber coated with P-selectin and ICAM-1 but does not affect choroidal neovascularization size following laser photocoagulation[6] It also has anti-inflammatory, angiogenic, and cardioprotective properties[7]

Isodunnianol exhibits anti-AChE activity with an IC50 value of 13.0 uM; it also exhibits neurite outgrowth-promoting activity at the concentration ranging from 0.1 to 10 uM in the primary cultured rat cortical neurons. Isodunnianol, dunnianol, and Macrant

Aristolactam BII exhibits antimicrobial and antiinflammatory activity, it shows significant activity towards DPPH radical scavenging and potent inhibitory effects against tyrosinase mushroom. Aristolactam BII also exerts its significant neuroprotective ef

LY836 is an orally active, neuroprotective compound that effectively inhibits the PSD95-nNOS association in cortical neurons. It has potential applications in the study of ischemic stroke [1].

Hydroxy-2-[2-(2-hydroxyphenyl)ethyl]chromone is a neuroprotective agent that exhibits marked neuroprotective activity by mitigating glutamate-induced neurotoxicity in primary rat cortical cell cultures [1].

[D-Arg25]-Neuropeptide Y (human) ([D-Arg25] NPY), a Y1 receptor selective agonist, plays a role in Alzheimer's disease (AD) and safeguards rat cortical neurons from β-Amyloid toxicity [1].

5,7-Dichlorokynurenic acid (5,7-dichlorokynurenic acid sodium) is an NMDA receptor antagonist.

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-Phe-L-Val) enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord following crush injury and of serotonin neurons in uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.

Pifithrin-α, p-Nitro, Cyclic (PFN-α) (PFN-α) is cell-permeable and active-form inhibitor of p53.

AR-A 2 is a selective 5-HT1B receptor antagonist, with a high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

Tat-βsyn-degron, an α-synuclein knockdown peptide, integrates three domains: the HIV-1 Tat plasma membrane transduction domain, an α-synuclein binding domain (βsyn) representing amino acids 36-45 of β-synuclein, and a proteasomal targeting domain (degron). It effectively binds to recombinant α-synuclein, demonstrating a significant reduction in α-synuclein levels in primary rat cortical neuron cultures.

CCK (26-30) is an N-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. The sulfated form of CCK (26-30) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 10% when used at a concentration of 0.1 mM.

Neuropeptide Y (29-64), amide, human (TFA) is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity.It is showed that Neuropeptide Y (29-64), amide, human (TFA) is able to protect cortical neurons from Aβ25-35 t

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

Forasartan is a non - peptide angiotensin II receptor antagonist with antihypertensive activity. Forasartan and angiotensin II compete to bind AT1 receptor subtypes in vascular smooth muscle, thereby blocking angiotensin II-mediated vasoconstriction, lead

N-methyl Paroxetine is a derivative of the selective serotonin reuptake inhibitor (SSRI) antidepressant paroxetine that inhibits [3H]paroxetine binding to rat cortical membranes (Ki = 4.3 nM). It inhibits serotonin uptake in rat brain synaptosomes with an IC50 value of 22 nM. N-methyl Paroxetine has been used as a precursor in the synthesis of paroxetine and is a potential impurity in commercial preparations of paroxetine.

Ac-RYYRWK-NH2 is a highly effective and specific partial agonist for the nociceptin receptor (NOP). It demonstrates a remarkable affinity for rat cortical membranes ORL1, with [3H]Ac-RYYRWK-NH2 exhibiting a Kd value of 0.071 nM. However, it shows negligible affinity towards μ-, κ-, or δ-opioid receptors.

Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices. Increases contralateral rotation in mice expressing PSAM4-GlyR unilaterally in the substantia nigra reticulata (LED 0.1 mg/kg). Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science 364 PMID:30872534

Dasycarpol(9beta-Hydroxyfraxinellone) shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cells at a concentration of 0.1 microM. Dasycarpol also shows moderate inhibitory activity on lung

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. Phenytoin potentially acts by promoting sodium efflux from neurons located in the motor cortex reducing post-tetanic potentiation at synapses. The reduction of potentiation prevents cortical seizure foci spreading to adjacent areas, stabilizing the threshold against hyperexcitability. In addition, this agent appears to reduce sensitivity of muscle spindles to stretch causing muscle relaxation.

VU0606170 is a slack channels inhibitor and was shown to successfully decrease the malfunctioning spontaneous firing rate of cortical neurons, providing a potential avenue for achieving an anti-epileptic effect not previously attainable.

Galnon is a galanin receptor agonist, improves intrinsic cortical bone tissue properties

1. Praeruptorin C has been widely used as an antioxidant and a calcium antagonist to treat diseases. 2. Praeruptorin C partially protects cortical neurons by inhibiting the expression of GluN2B-containing NMDA receptors and regulating the Bcl-2 family. 3.

MSN-125 effectively inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond

Pridopidine Hydrochloride is a dopaminergic stabilizer that has been shown to improve a variety of neurological and psychiatric disorders, including Huntington's disease. Pridopidine Hydrochloride stabilizes psychomotor activity in a state-dependent way t

LP-922056 is an inhibitor of Notum Pectinacetylesterase with EC50 values of 21 nM, 55 nM for human and mouse, respectively.

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

Hinokiresinol is a novel inhibitor of LTB4 binding to the human neutrophils, it has antiallergic effect, it inhibits IgE-induced mouse passive cutaneous anaphylaxis reaction. Hinokiresinol (trans-hinokiresinol) and nyasol (cis-hinokiresinol) are estrogen