brain membranes

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that 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; it can be used to study the central nervous system.

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].

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.

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

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

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).

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.

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).

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.

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).

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).

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

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

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

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.

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.

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.

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)

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.

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

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.

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.

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.