N-Acetylcysteine amide is a thiol antioxidant and neuroprotective agent that can permeate cell membranes and the blood-brain barrier.

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

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).

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice.(1R,2R)-2-PCCA hydrochloride can be used to study the central nervous system.

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

Omega-3 Arachidonic Acid ethyl ester, a rare polyunsaturated fatty acid with limited presence in dietary sources, is crucial for infant growth and development and offers protection against heart disease, blood clots, high blood pressure, and inflammatory and autoimmune disorders. In human platelet membranes, it impedes arachidonyl-CoA synthetase, exhibiting a Ki of 14 μM, and shows similar inhibitory effects on arachidonoyl-CoA synthetase in calf brain extract with an IC50 of roughly 5 μM. The ethyl arachidonate derivative offers enhanced lipophilicity compared to its free acid counterpart.

C22 Glucosylceramide (d18:1/22:0) is an endogenous glucosylceramide. Glucosylceramides are major constituents of skin lipid membranes where they play a role in maintaining the water permeability barrier. They are precursors in the synthesis of lactosylceramide , as well as oligoglycolipids and gangliosides. Phospholipase A2 (PLA2) type XIIA knockdown increases C22 glucosylceramide (d18:1/22:0) expression in rat brain. It is also increased in the brain, but not the liver or spinal cord, of mice fed a methionine-restricted diet. In human athletes, plasma levels of C22 glucosylceramide (d18:1/22:0) increase during exercise and return to basal levels during recovery. This product contains C22 glucosylceramide (d18:1/22:0) isolated from bovine buttermilk.

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.

C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. C18 globotriaosylceramide also accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease.

CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in mice when administered at doses up to 1 uMol/kg.

Sphingomyelins (SMs) are bioactive sphingolipids found in mammalian cell membranes.1SMs make up 2-15% of the total organ phospholipid population but are found at higher concentrations in the brain and myelin sheaths surrounding peripheral nerves. They interact with cholesterol to control its distribution within cellular membranes and maintain cholesterol homeostasis in cells. SMs undergo hydrolysis by sphingomyelinase to form ceramides, which are sphingolipid mediators of intracellular signaling.2This product is a mixture of SMs, with variable fatty acyl chain lengths, isolated from buttermilk. [Matreya, LLC. Catalog No. 1329] 1.Slotte, J.P., and Ramstedt, B.The functional role of sphingomyelin in cell membranesEur. J. Lipid Sci. Technol.109(10)977-981(2007) 2.Shayman, J.A.SphingolipidsKidney Int.58(1)11-26(2000)

Ganglioside GM2 is a glycosphingolipid component of cellular membranes, primarily the plasma membrane. Levels of ganglioside GM2 are elevated in the brain of patients with Sandhoff disease, as well as feline and mouse models of the disease. Ganglioside GM2 accumulates in the lysosomes of individuals with Tay-Sachs disease and GM2-activator deficiency, as well as in the CNS of patients with and animal models of mucopolysaccharide storage disorders and Niemann-Pick disease types A, C1, and C2. Ganglioside GM2 mixture contains ganglioside GM2 molecular species with C18:1 and C20:1 sphingoid backbones.

Endosulfan I is an organochlorine insecticide and a stereoisomer of endosulfan II . It is active against a variety of insects, including bollworms (LD50 = 0.63 mg/g). Endosulfan I binds to GABA receptors in rat brain membranes with an IC50 value of 30 nM and is toxic to rats (LD50 = 18 mg/kg).

L-701324 is an NMDA receptor with high affinity and selectivity for the glycine site, used as an orally active and long-acting anticonvulsant.

Preincubation of guinea pig brain membranes with BTCP was shown to produce an increase in the dissociation rate of [3H]TCP from PCP site。

(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium. It is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes

Z-Glycine (Carbobenzoxyglycine) is a drug-lipid conjugates designed to promote brain penetration based on its lipophilicity and resemblance to lipids in biological membranes[1].

GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronch

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

Cyclocreatine, a Creatine analogue, exhibits potent bioenergetic protection by elevating ATP levels. It demonstrates the ability to traverse cell membranes, including the blood-brain barrier, wherein it undergoes phosphorylation and dephosphorylation by creatine kinases.

Phosphatidylethanolamine is the most abundant phospholipid in prokaryotes and the second most abundant found in the membrane of mammalian, plant, and yeast cells, comprising approximately 25% of total mammalian phospholipids. In the brain, phosphatidylethanolamine comprises almost half of the total phospholipids. It is synthesized mainly through the cytidine diphosphate-ethanolamine and phosphatidylserine decarboxylation pathways, which occur in the endoplasmic reticulum (ER) and mitochondrial membranes, respectively. It is a precursor in the synthesis of phosphatidylcholine and arachidonoyl ethanolamide and is a source of ethanolamine used in various cellular functions. In E. coli, phosphatidylethanolamine deficiency prevents proper assembly of lactose permease, suggesting a role as a lipid chaperone. It is a cofactor in the propagation of prions in vitro and can convert recombinant mammalian proteins into infectious molecules even in the absence of RNA. Phosphatidylethanolamines (soy) is a mixture of phosphatidylethanolamines isolated from soy with various fatty acyl groups at the sn-1 and sn-2 positions.

Sphingomyelins (SMs) are bioactive sphingolipids present in the cell membranes of mammals, constituting 2-15% of the total cellular phospholipid content, with higher concentrations in the brain and myelin sheaths of peripheral nerves. These compounds play a crucial role in modulating cholesterol distribution and maintaining cellular cholesterol balance. SMs are hydrolyzed by sphingomyelinase into ceramides, key sphingolipid signaling molecules. The product contains SM species predominantly with C16:0 fatty acyl chain lengths and may exhibit variations in its sphingoid backbone due to its natural origin. [Matreya, LLC. Catalog No. 1332]

N-Carbobenzyloxyglycine-d2 is a deuterated compound of N-Carbobenzyloxyglycine. N-Carbobenzyloxyglycine has a CAS number of 1138-80-3. Z-Glycine (Carbobenzoxyglycine) is a drug-lipid conjugates designed to promote brain penetration based on its lipophilicity and resemblance to lipids in biological membranes[1].

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.

8-CSC is a dual agent endowed with good hMAO-B inhibitory activity (Ki: 235 nM in baboon liver mitochondria) and A2A affinity (Ki: 36 nM in rat brain striatal membranes receptor).

Levomefolate magnesium is the magnesium salt of the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma. It is transported across th

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.

PBT434 is a novel, brain-penetrant, small molecule inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin.

Phosphatidylethanolamines (bovine) are a mixture of phosphatidylethanolamines isolated from bovine brain with different fatty acyl groups at the sn-1 and sn-2 positions.Phosphatidylethanolamines (bovine) are the most abundant phospholipids in prokaryotes and the second most abundant in mammalian, plant and yeast cell membranes. Phosphatidylethanolamines (bovine) are the most abundant phospholipids in prokaryotes and the second most abundant phospholipids in the cell membranes of mammals, plants, and yeast, accounting for about 25% of the total mammalian phospholipids.

PD 122860 is a dihydropyridine with calcium channel blocking and sodium channel stimulating properties. In the rat heart, PD 122860 increased left ventricular contractility, decreased coronary resistance and altered the shape of the electrocardiogram T-wa

[DAla4] Substance P (4-11), an analog of Substance P (Substance P), effectively inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (Eledoisin) and 125I-Bolton Hunter-conjugated Substance P to rat brain cortex membranes, with IC50 values of 0.5 μM and 0.15 μM, respectively [1].

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA B receptor agonist with an EC 50 of 8.6 nM for human recombinant GABA B receptor. The affinity ( K i s) of Lesogaberan hydrochloride for rat GABA B and GABA A receptors, as measured by displacement of GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .

(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

Kojic amine is a GABA receptor agonist; potent and specific inhibitor of Na+-independent GABA binding to rat brain membranes.

SCH-37370 is an effective and orally active dual antagonist of platelet-activating factor and histamine. Sch 37370 blocks the binding of [3H]pyrilamine to histamine-H1 receptors in rat brain membranes. Sch 37370 selectively inhibits PAF-induced aggregation of human platelets (IC50 : 0.6 mM) and also competes with PAF binding to specific sites in membrane preparations from human lungs (IC50 : 1.2 mM).

Methylatropine is an antagonist of muscarinic acetylcholine receptors (IC50= <0.1 nM in a radioligand binding assay using isolated porcine brain membranes) and a derivative of atropine .1,2It reduces acetylcholine-induced decreases in blood pressure in rats when administered intravenously with an ED50value of 5.5 μg/kg.2Methylatropine reduces salivation, induces mydriasis, and increases heart rate in dogs.3 1.Schmeller, T., Sporer, F., Sauerwein, M., et al.Binding of tropane alkaloids to nicotinic and muscarinic acetylcholine receptorsPharmazie50(7)493-495(1995) 2.Brezenoff, H.E., Xiao, Y.-F., and Vargas, H.A comparison of the central and peripheral antimuscarinic effects of atropine and methylatropine injected systemically and into the cerebral ventriclesLife Sci.42(8)905-911(1988) 3.Albanus, L.Central and peripheral effects of anticholinergic compoundsActa Pharmacol. Toxicol. (Copenh)28(4)305-326(1970)

ShK toxin, isolated from the Caribbean sea anemone (Stichodactyla helianthus), is an inhibitor of the voltage-dependent potassium channel (Kv1.3 channel). It competes with dendrotoxin I and α-dendrotoxin in binding to rat brain synaptosomal membranes and promotes acetylcholine release. Additionally, ShK toxin reduces K+ currents in cultured rat dorsal root ganglion neurons and inhibits T lymphocyte proliferation [1] [2].

KS 5-2 has affinity to isolated synaptic membranes from rat brain.

Ganglioside GD1b is an acidic glycosphingolipid that contains two sialic acid residues linked to an inner galactose unit. It is a component of plasma membranes where it packs densely with cholesterol to form lipid microdomains that modulate both intra- and intercellular signaling events. The concentration of ganglioside GD1b in human brain increases with age, constituting 7.85% of total sialic acid in the brain of 0- to 10-year-old subjects and 20.29% in 11- to 30-year-old subjects. Ganglioside GD1b mixture contains ganglioside GD1b molecular species with C18:1 and C20:1 fatty acyl chains.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).

L-736380 is a CCK-B receptor antagonist. L-736,380 dose-dependently inhibited gastric acid secretion in anesthetized rats (ID(50), 0.064 mg/kg) and ex vivo binding of [(125)I]CCK-8S in BKTO mice brain membranes (ED(50), 1.7 mg/kg).

Dizocilpine Maleate (MK 801) is a potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) with Kd of 37.2 nM in rat brain membranes. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role.

Endosulfan II, an organochlorine insecticide and a stereoisomer of Endosulfan I, effectively targets various insects such as bollworms and tobacco budworms, with lethal doses (LD50s) of 4.14 and 4.95 mg/g, respectively. It interacts with GABA receptors in rat brain membranes, demonstrating an inhibition concentration (IC50) of 60 nM. Notably, Endosulfan II exhibits lower toxicity in rats compared to Endosulfan I, with LD50 values of 240 and 18 mg/kg, respectively.

Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.

5-hydroxy Isatin is an inhibitor of monoamine oxidase A and also inhibits atrial natriuretic peptide-induced activation of particulate guanylyl cyclase in rat brain and heart membranes.

CCK (26-31) 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 (26-31) inhibits binding of [125I]CCK-33 to guinea pig cortical membranes by 21% when used at a concentration of 0.1 mM.