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brain membranes

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  • Inhibitors & Agonists
    46
    TargetMol | Inhibitors_Agonists
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    8
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(1R,2R)-2-PCCA hydrochloride
(1R,2R)-2-PCCA(hydrochloride)
T134231609563-71-4In house
(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.
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6-8 weeks
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5-HT3 antagonist 3
T10162120635-47-4In house
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).
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6-8 weeks
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Phosphatidylethanolamine from bovine
T3814090989-93-8
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.
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Z-Glycine
N-Carbobenzoxyglycine, Carbobenzoxyglycine
T336041138-80-3
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].
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DPCPX
PD 116948
T22744102146-07-6
DPCPX (PD 116948) is an A1 adenosine receptor antagonist
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TargetMol | Citations Cited
SR 57227 hydrochloride
SR 57227A, SR 57227 hydrochloride
T2339477145-61-0
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.
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SCH-37370
T19686117796-52-8
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).
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L-701324
L701324
T1909142326-59-8
L-701324 is an NMDA receptor with high affinity and selectivity for the glycine site, used as an orally active and long-acting anticonvulsant.
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JW 642
T156321416133-89-5
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).
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Ac-RYYRIK-NH2 acetate
TP1940L1
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.
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C22 Glucosylceramide (d18:1/22:0)
T38282119242-44-3
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.
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35 days
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N-methyl Paroxetine
T35920110429-36-2
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.
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CCK (26-30) (sulfated)
T3720389911-69-3
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.
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8-CSC
8 CSC,CSC
T23587148589-13-3
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).
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6-8 weeks
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Levomefolate magnesium
L-Methylfolate magnesium
T327051429498-11-2
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
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N-Carbobenzyloxyglycine-d2
TMIJ-0079
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].
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20 days
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PBT434 HBr
T711741232841-78-9
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.
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8-10 weeks
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Aselacin A
TN9071156223-06-2
Aselacin A targets the endothelin-1 receptor (ET-1 Receptor) and inhibits the binding of ET-1 to both ETA and ETB receptors. It effectively impedes the binding of ET-1 to bovine atrial membranes and porcine brain membranes, with IC50 values of 22 μg mL and 20 μg mL, respectively. Aselacin A is applicable for cardiovascular disease research.
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omega-3 Arachidonic acid ethyl ester
ω-3 Arachidonic acid ethyl ester, (all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester
T81609123940-93-2
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.
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8-10 weeks
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tandospirone
SM-3997, SM3997
TQ031587760-53-0
Tandospirone (SM-3997) is a selective and potent 5-HT1A receptor partial agonist with anxiolytic and antidepressant activity that potentiates the anticardiac fibrotic effect of valsartan in spontaneously hypertensive rats, and can be used in the study of central nervous system disorders.
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7-10 days
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C18 Globotriaosylceramide (d18:1/18:0)
T3743969283-33-6
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.
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CCK (27-33) (non-sulfated)
T3720647910-79-2
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.
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Sphingomyelins (buttermilk)
T37953475662-40-9
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)
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PD 122860
PD-122860,PD122860
T28321122576-86-7
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
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6-8 weeks
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