brain membranes

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

Carabersat(SB 204269) is a novel and effective anticonvulsant and antiepileptic agent.

DPCPX (PD 116948) is an A1 adenosine receptor antagonist

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.

Cyclocreatine, a creatine analogue and substrate for creatine kinase, inhibits creatine metabolism and prostate cancer cell proliferation, improving cognitive, autistic and epileptic phenotypes in mouse models of creatine transporter deficiency (CTD).

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).

S1PR5-IN-1 (Compound 7a) is a selective S1PR5 inhibitor capable of crossing the blood-brain barrier, with an IC50 of 85.4 nM. It exhibits exceptional binding affinity to S1PR5, with Kd values of 2.2 nM for recombinant human S1PR5 cell membranes, 4.6 nM for C57BL/6 mouse brains, and 27.6 nM for human cerebral cortex. S1PR5-IN-1 is applicable in researching neurodegenerative diseases such as multiple sclerosis.

Claramine hydrochloride is a steroidal polyamine capable of crossing the blood-brain barrier. It modulates the properties of lipid membranes and safeguards cells against various biological toxins, including misfolded protein oligomers and bio-protein toxins.

Quinidine methiodide is a quaternized derivative of quinidine and a classical ion channel blocker. Unable to penetrate the blood-brain barrier, it prolongs action potential duration by exclusively blocking voltage-gated sodium and potassium channels on peripheral membranes, acting as a benchmark tool in neuromuscular and cardiovascular electrophysiology research.

AChE/BChE-IN-35, a tacrine derivative, is a dual inhibitor of AChE and BChE capable of crossing the blood-brain barrier. It exhibits an IC50 of 123.66 nM for electric eel AChE, 122.34 nM for human AChE, and 488.00 nM for equine BChE. The compound crosses cell membranes through LAT1-mediated active transport, showing increased brain exposure and a slower clearance rate from brain tissue. AChE/BChE-IN-35 is applicable in Alzheimer's disease research.

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 maleate) is a potent, selective, and non-competitive NMDA receptor antagonist with a Kd value of 37.2 nM. It is commonly used in the treatment of various neurodegenerative diseases in which NMDA receptors may be involved, and can also be used to induce schizophrenia models.

Epsilon-V1-2 has been extensively investigated for its function as a PKC epsilon (PKCε) inhibitor. Epsilon-V1-2 has been widely applied in studies addressing ovarian aging, apoptosis in human granulosa cells, cerebral ischemia-reperfusion injury, brain development, hepatocyte insulin signaling, and neuronal cell death under ischemic conditions. Epsilon-V1-2 has been shown to effectively reduce PKCε activity, thereby enabling detailed exploration of regulatory pathways involving mitochondrial dynamics, calcium overload, AKT activation, brain atrophy, insulin resistance, and ferroptosis. Epsilon-V1-2 demonstrates notable therapeutic relevance in models of stroke, SHORT syndrome, hepatic steatosis, and brain injury, supporting its continued evaluation as a potential pharmacological agent across multiple disease contexts.

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.