ArticleJournal of molecular neuroscience : MN1998
Substituted cGMP analogs can act as selective agonists of the rod photoreceptor cGMP-gated cation channel.
Article in Journal of molecular neuroscience : MN, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 55 citations in OpenAlex.
- Rod photoreceptors have a dual dependency on both aerobic glycolysis and OXPHOS and diverge metabolically from other retinal neurons.Science advances · 2026Article
- PDE5A Inhibition Restricts Cancer Metastasis by Disrupting NPC1-Mediated Cholesterol Trafficking through a Noncanonical cGMP-Dependent Pathway.Cancer research · 2026Article
- Similar Binding Modes of cGMP Analogues Limit Selectivity in Modulating Retinal CNG Channels via the Cyclic Nucleotide-Binding Domain.ACS chemical neuroscience · 2024Article
- C-type natriuretic peptide promotes adipogenic differentiation of goat adipose-derived stem cells via cGMP/PKG/ p38 MAPK signal pathway.In vitro cellular & developmental biology. Animal · 2021Article
- Fluorophore-Labeled Cyclic Nucleotides as Potent Agonists of Cyclic Nucleotide-Regulated Ion Channels.Chembiochem : a European journal of chemical biology · 2020Article
- Hydrophobic alkyl chains substituted to the 8-position of cyclic nucleotides enhance activation of CNG and HCN channels by an intricate enthalpy - entropy compensation.Scientific reports · 2018Article
- Establishing a Split Luciferase Assay for Proteinkinase G (PKG) Interaction Studies.International journal of molecular sciences · 2018Article
- Cyclic nucleotide-gated channels, calmodulin, adenylyl cyclase, and calcium/calmodulin-dependent protein kinase II are required for late, but not early, long-term memory formation in the honeybee.Learning & memory (Cold Spring Harbor, N.Y.) · 2014Article
- Article
- Disease-associated mutations in CNGB3 promote cytotoxicity in photoreceptor-derived cells.Molecular vision · 2013Article
- Light-driven calcium signals in mouse cone photoreceptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- Effects of cyclic nucleotide-gated channels in vestibular nuclear neurons.Chonnam medical journal · 2011Article
- Hyperpolarization-activated ion channels as targets for nitric oxide signalling in deep cerebellar nuclei.The European journal of neuroscience · 2010Article
- Article
- Gonadotropin-releasing hormone-1 neuronal activity is independent of cyclic nucleotide-gated channels.Endocrinology · 2008Article
- Novel N7- and N1-substituted cGMP derivatives are potent activators of cyclic nucleotide-gated channels.Journal of medicinal chemistry · 2007Article
- The pharmacology of cyclic nucleotide-gated channels: emerging from the darkness.Current pharmaceutical design · 2006Review
- The limit of photoreceptor sensitivity: molecular mechanisms of dark noise in retinal cones.The Journal of general physiology · 2005Article
- AMPA receptor activates a G-protein that suppresses a cGMP-gated current.The Journal of neuroscience : the official journal of the Society for Neuroscience · 1999Article
- Pseudechetoxin: a peptide blocker of cyclic nucleotide-gated ion channels.Proceedings of the National Academy of Sciences of the United States of America · 1999Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
Cyclic nucleotide-gated (CNG) channels are expressed in many cell types in both the nervous system and nonexcitable tissues. In order to understand the roles of cGMP-gated channels, and to distinguish actions of cGMP mediated through CNG channels from those through cGMP-dependent protein kinase (G-kinase), several new cGMP analogs were tested for potency as CNG channel agonists. Using Xenopus oocytes expressing the rat rod cGMP-gated ion channel alpha-subunit, we showed that an analog containing a pCPT group at the 8-position, 8-pCPT-cGMP, was 80 times more potent than cGMP and 14 times more potent than 8-Br-cGMP. 8-pCPT-cGMP is the most potent CNG channel agonist so far described and also has the advantages of much better membrane permeability as well as much higher resistance to PDE-hydrolysis, as compared with 8-Br-cGMP. Modification of both 8-Br-cGMP and 8-pCPT-cGMP by introduction of a sulphur atom into the cyclic phosphate group gave smaller changes in agonist efficiency. Both Sp-8-Br-cGMPS and Sp-8-pCPT-cGMPS acted as agonists of CNG channels and are also G-kinase activators. In contrast, Rp-8-Br-cGMPS was a channel agonist, with an EC50 of 173.5 microM, but a G-kinase antagonist with a Ki of 4 microM. Finally, Rp-8-pCPT-cGMPS was a channel agonist and showed additional noncompetitive antagonist activity at higher concentrations. 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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.