ArticleBritish journal of pharmacology2012
Inhibition of human recombinant T-type calcium channels by N-arachidonoyl 5-HT.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
11 citing papers in PubMed, 18 citations in OpenAlex.
- Modulation of Recombinant Human T-Type Calcium Channels by ΔCannabis and cannabinoid research · 2022Article
- Analgesic transient receptor potential vanilloid-1-active compounds inhibit native and recombinant T-type calcium channels.British journal of pharmacology · 2019Article
- Regulation of heterologously expressed 5-HTBritish journal of pharmacology · 2019Article
- New approaches and challenges to targeting the endocannabinoid system.Nature reviews. Drug discovery · 2018Review
- Targeting voltage-gated calcium channels in neurological and psychiatric diseases.Nature reviews. Drug discovery · 2016Review
- NMP-7 inhibits chronic inflammatory and neuropathic pain via block of Cav3.2 T-type calcium channels and activation of CB2 receptors.Molecular pain · 2014Article
- 5,6-EET potently inhibits T-type calcium channels: implication in the regulation of the vascular tone.Pflugers Archiv : European journal of physiology · 2014Article
- Oxidation of endogenous N-arachidonoylserotonin by human cytochrome P450 2U1.The Journal of biological chemistry · 2014Article
- Modulation of T-type calcium channels by bioactive lipids.Pflugers Archiv : European journal of physiology · 2014Review
- Article
- Analgesic effect of a mixed T-type channel inhibitor/CB2 receptor agonist.Molecular pain · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeN-arachidonoyl 5-HT (NA-5HT) has anti-nociceptive effects reported to be mediated by inhibitory actions at the transient receptor potential vanilloid receptor 1 (TRPV1) and fatty acid amide hydrolase (FAAH). Anandamide and N-arachidonoyl dopamine (NA-DA), endocannabinoids that activate TRPV1 or are metabolized by FAAH, also inhibit T-type calcium channels (I(Ca) ). T-type I(Ca) are expressed by many excitable cells, including neurons involved in pain detection and processing. We sought to determine whether NA-5HT also modulates T-type I(Ca) . EXPERIMENTAL APPROACH: Human recombinant T-type I(Ca) (Ca(V) 3 channels) expressed in HEK 293 cells were examined using standard whole-cell voltage-clamp electrophysiology techniques. KEY
resultsNA-5HT completely inhibited Ca(V) 3 channels with a rank order of potency (pEC(50) ) of Ca(V) 3.1 (7.4) > Ca(V) 3.3 (6.8) ≥ Ca(V) 3.2 (6.6). The effects of NA-5HT were voltage-dependent, and it produced significant hyperpolarizing shifts in Ca(V) 3 steady-state inactivation relationships. NA-5HT selectively affected Ca(V) 3.3 channel kinetics. CONCLUSIONS AND IMPLICATIONS: NA-5HT increases the steady-state inactivation of Ca(V) 3 channels, reducing the number of channels available to open during depolarization. These effects occur at NA-5HT concentrations at or below those at which NA-5HT affects TRPV1 receptors and FAAH. NA-5HT is one of the most potent inhibitors of T-type I(Ca) described to date, and it is likely to exert some of its biological effects, including anti-nociception, via inhibition of these channels.
Indexed as
Identifiers
What OpenQuestion holds
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.