2-APB - CAS 524-95-8
Category: Inhibitor
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TRP Channel
2-APB, a transient receptor potential (TRP) activator for TRPV1, TRPV2, and TRPV3, could probably be used against diseases caused by hypersensitivity and temperature misregulation.
≥98% by HPLC
White Solid
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1.IP(3) receptor antagonist, 2-APB, attenuates cisplatin induced Ca2+-influx in HeLa-S3 cells and prevents activation of calpain and induction of apoptosis.
Splettstoesser F;Florea AM;Büsselberg D Br J Pharmacol. 2007 Aug;151(8):1176-86. Epub 2007 Jun 25.
BACKGROUND AND PURPOSE: ;Cisplatin drives specific types of tumour cells to apoptosis. In this study we investigate the involvement of intracellular calcium ([Ca(2+)](i)) in triggering apoptosis in two different cell lines. As cisplatin is used for the treatment of several forms of cancer we choose HeLa-S3 and U2-OS as two examples of tumour cell lines.;EXPERIMENTAL APPROACH: ;Cisplatin (1 nM-10 microM) was applied to HeLa-S3 and U2-OS cells and [Ca(2+)](i) measured with fluo-4, using laser scanning microscopy. Inositol-1,4,5-trisphosphate (IP(3)) receptors were visualized with immunostaining. Membrane conductances were measured with patch-clamp techniques. Levels of calpain and caspases were assessed by western blots and apoptotic cells were stained with Hoechst 33342 and counted.;KEY RESULTS: ;Cisplatin increases [Ca(2+)](i) concentration-dependently in HeLa-S3 but not in U2-OS cells. This elevation of [Ca(2+)](i) depended on extracellular Ca(2+) but was reduced by the IP(3) receptor blocker, 2-APB. This effect was not due to a Ca(2+) release triggered by Ca(2+) entry. Immunostaining showed IP(3)-receptors (type 1-3) at the cellular membrane of HeLa-S3 cells, but not in U2-OS cells.
2.Enhanced transient receptor potential channel-mediated Ca
Murakami K;Osanai T;Tanaka M;Nishizaki K;Kinjo T;Tanno T;Ishida Y;Suzuki A;Endo T;Tomita H;Okumura K Fundam Clin Pharmacol. 2017 Aug;31(4):383-391. doi: 10.1111/fcp.12269. Epub 2017 Feb 16.
We reported that coronary spasm was induced in the transgenic mice with the increased phospholipase C (PLC)-δ1 activity. We investigated the effect of enhanced PLC-δ1 on Ca;2+; influx and its underlying mechanisms. We used human embryonic kidney (HEK)-293 and coronary arteries smooth muscle cells (CASMC). Intracellular free Ca;2+; concentration ([Ca;2+; ];i; ; nm) was measured by fura-2, and Ca;2+; influx was evaluated by the increase in [Ca;2+; ];i; after addition of extracellular Ca;2+; . Acetylcholine (ACh) was used to induce Ca;2+; influx. ACh-induced peak Ca;2+; influx was 19 ± 3 in control HEK-293 cells and 71 ± 8 in the cells with PLC-δ1 overexpression (P < 0.05 between two groups). Nifedipine partially suppressed this Ca;2+; influx, whereas either 2-APB or knockdown of classical transient receptor potential channel 6 (TRPC6) blocked this Ca;2+; influx. In the human CASMC, ACh-induced peak Ca;2+; influx was 29 ± 6 in the control and was increased to 45 ± 16 by PLC-δ1 overexpression (P < 0.05). Like HEK-293 cells, pretreatment with nifedipine partially suppressed Ca;2+; influx, whereas either 2-APB or knockdown of TRPC6 blocked it. ACh-induced Ca;2+; influx was enhanced by PLC-δ1 overexpression, and was blocked partially by nifedipine and completely by 2-APB.
3.Circulating Neurotoxic 5-HT2A Receptor Agonist Autoantibodies in Adult Type 2 Diabetes with Parkinson's Disease.
Zimering MB J Endocrinol Diabetes. 2018;5(2). doi: 10.15226/2374-6890/5/2/01102. Epub 2018 May 10.
Aims: ;To test whether circulating neurotoxic autoantibodies increase in adult type 2 diabetes mellitus with Parkinson's disease (PD) or dementia. To identify the G-protein coupled receptor on neuroblastoma cells mediating neural inhibitory effects in diabetic Parkinson's disease plasma autoantibodies. To determine the mechanism of accelerated neuroblastoma cell death and acute neurite retraction induced by diabetic Parkinson's disease and dementia autoantibodies.;Methods: ;Protein-A eluates from plasma of twelve older adult male diabetic patients having Parkinson's disease (n=10) or dementia (n=2), and eight age-matched control diabetic patients were tested for ability to cause accelerated N2A neuroblastoma cell death and acute neurite retraction. Specific antagonists of G protein coupled receptors belonging to the G alpha q subfamily of heterotrimetric G-proteins, the phospholipase C/inositol triphosphate/Ca2+ pathway, or the RhoA/Rho kinase pathway were tested for ability to block diabetic Parkinson's disease/dementia autoantibody-induced neurite retraction or N2A accelerated cell loss. Sequential Liposorber LA-15 dextran sulfate cellulose/protein-A affinity chromatography was used to obtain highly-purified fractions of diabetic Parkinson's disease autoantibodies.
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CAS 524-95-8 2-APB

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