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Chemical Compound Review

AC1MI02F     (2R,5R)-2-(2-amino-8-bromo- purin-9-yl)-5...

Synonyms: 8-Br-Cgmps
 
 
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Disease relevance of Rp-8-Br-Cgmps

  • In addition, KT5823 (1 nmol) or Rp-8-bromoguanosine-3':5'-cyclic monophosphothioate (Rp-8-Br-cGMPS; 1 nmol), an inhibitor of cyclic GMP-dependent protein kinase, also significantly suppressed BK-induced hyperalgesia [1].
 

High impact information on Rp-8-Br-Cgmps

  • The cGMP-dependent protein kinase inhibitor Rp-8-Br-cGMPS completely inhibited the effects of ANP and BNP [2].
  • The shift by 8-Br-cAMP as well as by 8-Br-cGMP was completely reversed by Rp-8-Br-cGMPS, while a selective inhibitor of activation of cAMP-kinase, (Rp)-adenosine-3',5'-cyclic monophosphorothioate (Rp-cAMPS), was without effects on the shift produced by these two compounds [3].
  • The results suggest that 8-pCPT-cGMPS is a highly potent photoreceptor CNG channel agonist with high membrane permeability and PDE-resistance and furthermore Rp-8-Br-cGMPS can be used to test whether the actions of cGMP are selectively mediated by CNG channels [4].
  • The NO donor diethylamine NONOate (DEANO), the PKG activator 8-pCPT-cGMP, and the PDE-5 inhibitor sildenafil, cause dose-dependent clitoral relaxation that is inhibited by antagonists of PKG (Rp-8-Br-cGMPS) or BK(Ca) channels (iberiotoxin) [5].

References

  1. Involvement of endogenous nitric oxide in the mechanism of bradykinin-induced peripheral hyperalgesia. Nakamura, A., Fujita, M., Shiomi, H. Br. J. Pharmacol. (1996) [Pubmed]
  2. Natriuretic peptides modulate nitric oxide synthesis in cytokine-stimulated cardiac myocytes. Yamamoto, K., Ikeda, U., Shimada, K. J. Mol. Cell. Cardiol. (1997) [Pubmed]
  3. cGMP-kinase mediates cGMP- and cAMP-induced Ca2+ desensitization of skinned rat artery. Kawada, T., Toyosato, A., Islam, M.O., Yoshida, Y., Imai, S. Eur. J. Pharmacol. (1997) [Pubmed]
  4. Substituted cGMP analogs can act as selective agonists of the rod photoreceptor cGMP-gated cation channel. Wei, J.Y., Cohen, E.D., Genieser, H.G., Barnstable, C.J. J. Mol. Neurosci. (1998) [Pubmed]
  5. The neurovascular mechanism of clitoral erection: nitric oxide and cGMP-stimulated activation of BKCa channels. Gragasin, F.S., Michelakis, E.D., Hogan, A., Moudgil, R., Hashimoto, K., Wu, X., Bonnet, S., Haromy, A., Archer, S.L. FASEB J. (2004) [Pubmed]
 
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