The DOI matches its Crossref record; 32 of the 32 references it cites were found in a registry or an index.
Block of TRPC5 channels by 2‐aminoethoxydiphenyl borate: a differential, extracellular and voltage‐dependent effect
Open accessAbstract
2‐Aminoethoxydiphenyl borate (2‐APB) has been widely used to examine the roles of inositol 1,4,5‐trisphosphate receptors (IP 3 Rs) and store‐operated Ca 2+ entry and is an emerging modulator of cationic channels encoded by transient receptor potential (TRP) genes. Using Ca 2+‐indicator dye and patch‐clamp recording we first examined the blocking effect of 2‐APB on human TRPC5 channels expressed in HEK‐293 cells. The concentration–response curve has an IC 50 of 20 μM and slope close to 1.0, suggesting one 2‐APB molecule binds per channel. The blocking effect is not shared by other Ca 2+ channel blockers including methoxyverapamil, nifedipine, N‐propargylnitrendipine, or berberine. In whole‐cell and excised membrane patch recordings, 2‐APB acts from the extracellular but not intracellular face of the membrane. Block of TRPC5 by 2‐APB is less at positive voltages, suggesting that it enters the electric field or acts by modulating channel gating. 2‐APB also blocks TRPC6 and TRPM3 expressed in HEK‐293 cells, but not TRPM2. Block of TRP channels by 2‐APB may be relevant to cell proliferation because 2‐APB has a greater inhibitory effect on proliferation in cells overexpressing TRPC5. Our data indicate a specific and functionally important binding site on TRPC5 that enables block by 2‐APB. The site is only available via an extracellular route and the block shows mild voltage‐dependence. British Journal of Pharmacology (2005) 145, 405–414. doi:10.1038/sj.bjp.0706197
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Cites
TRP channels as cellular sensors
Clapham, D. E. (2003) · Nature · doi:10.1038/nature02196 · Cited by 2,779
ADP-ribose gating of the calcium-permeable LTRPC2 channel revealed by Nudix motif homology
Perraud, A.-L., Fleig, A., Dunn, C. A., Bagley, L. A., Launay, P., Schmitz, C., Stokes, A. J., Zhu, Q., Bessman, M. J., Penner, R., et al. (2001) · Nature · doi:10.1038/35079100 · Cited by 892
TRPC1 and TRPC5 Form a Novel Cation Channel in Mammalian Brain
Strübing, C., Krapivinsky, G., Krapivinsky, L., & Clapham, D. E. (2001) · Neuron · doi:10.1016/s0896-6273(01)00240-9 · Cited by 738
Polycystin-2 is an intracellular calcium release channel
Koulen, P., Cai, Y., Geng, L., Maeda, Y., Nishimura, S., Witzgall, R., Ehrlich, B. E., & Somlo, S. (2002) · Nature Cell Biology · doi:10.1038/ncb754 · Cited by 706
Bootman, M. D., Collins, T. J., Mackenzie, L., Roderick, H. L., Berridge, M. J., & Peppiatt, C. M. (2002) · The FASEB Journal · doi:10.1096/fj.02-0037rev · Cited by 692
Requirement of the Inositol Trisphosphate Receptor for Activation of Store-Operated Ca 2+ Channels
Ma, H.-T., Patterson, R. L., van, D. B., Rossum, Birnbaumer, L., Mikoshiba, K., & Gill, D. L. (2000) · Science · doi:10.1126/science.287.5458.1647 · Cited by 577
2-Aminoethoxydiphenyl Borate Is a Common Activator of TRPV1, TRPV2, and TRPV3
Hu, H.-Z., Gu, Q., Wang, C., Colton, C. K., Tang, J., Kinoshita-Kawada, M., Lee, L.-Y., Wood, J. D., & Zhu, M. X. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m404164200 · Cited by 517
Prakriya, M., & Lewis, R. S. (2001) · The Journal of Physiology · doi:10.1111/j.1469-7793.2001.t01-1-00003.x · Cited by 493
TRPC5 is a regulator of hippocampal neurite length and growth cone morphology
Greka, A., Navarro, B., Oancea, E., Duggan, A., & Clapham, D. E. (2003) · Nature Neuroscience · doi:10.1038/nn1092 · Cited by 382
Molecular and Functional Characterization of the Melastatin-related Cation Channel TRPM3
Grimm, C., Kraft, R., Sauerbruch, S., Schultz, G., & Harteneck, C. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m300945200 · Cited by 367
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Metadata
- Authors
- Xu, S., Zeng, F., Boulay, G., Grimm, C., Harteneck, C., & Beech, D. J.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2005-06
- Volume
- 145
- Issue
- 4
- Pages
- 405-414
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W1840415699
- Cited by
- 258
- References
- 32
- FWCI
- 7.04
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Xu, S., Zeng, F., Boulay, G., Grimm, C., Harteneck, C., & Beech, D. J. (2005). Block of TRPC5 channels by 2‐aminoethoxydiphenyl borate: a differential, extracellular and voltage‐dependent effect. British Journal of Pharmacology. https://doi.org/10.1038/sj.bjp.0706197
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