ArticleBMC pharmacology2004
A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats.
Article in BMC pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers, 1 of them a synthesis that pooled it.
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
31 citing papers in PubMed, 1 synthesis or guideline pooled it, 95 citations in OpenAlex.
- Efficacy of pregabalin and gabapentin for neuropathic pain in spinal-cord injury: an evidence-based evaluation of the literature.European journal of clinical pharmacology · 2008Pooled it
- Effects of Gabapentinoids Premedication on Shoulder Pain and Rehabilitation Quality after Laparoscopic Cholecystectomy: Pregabalin versus Gabapentin.Pain research & management · 2018Trial
- Consensus on the Clinical Use of Pregabalin in Peripheral Neuropathic Pain.CNS neuroscience & therapeutics · 2026Review
- Pharmacological and Nonpharmacological Treatments for Painful Diabetic Peripheral Neuropathy.Diabetes & metabolism journal · 2023Review
- Pregabalin for chemotherapy-induced neuropathy: background and rationale for further study.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 2022Review
- High dose gabapentin does not alter tumor growth in mice but reduces arginase activity and increases superoxide dismutase, IL-6 and MCP-1 levels in Ehrlich ascites.BMC research notes · 2019Article
- Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels.Molecular pharmacology · 2018Article
- Analgesic effects of a hydro-ethanolic whole plant extract of Synedrella nodiflora (L.) Gaertn in paclitaxel-induced neuropathic pain in rats.BMC research notes · 2017Article
- Comparative effects of chronic administrations of gabapentin, pregabalin and baclofen on rat memory using object recognition test.Research in pharmaceutical sciences · 2017Article
- Pregabalin in neuropathic pain: evidences and possible mechanisms.Current neuropharmacology · 2014Article
- Modulation of voltage-gated Ca2+ channels in rat retinal ganglion cells by gabapentin.Visual neuroscience · 2014Article
- Pregabalin abuse and dependence in Germany: results from a database query.European journal of clinical pharmacology · 2013Article
- Gabapentin and (S)-pregabalin decrease intracellular D-serine concentrations in PC-12 cells.Neuroscience letters · 2013Article
- Pregabalin suppresses nociceptive behavior and central sensitization in a rat trigeminal neuropathic pain model.The journal of pain · 2013Article
- Pregabalin attenuates excitotoxicity in diabetes.PloS one · 2013Article
- Gabapentin inhibits catecholamine release from adrenal chromaffin cells.Anesthesiology · 2012Article
- Riluzole and gabapentinoids activate glutamate transporters to facilitate glutamate-induced glutamate release from cultured astrocytes.European journal of pharmacology · 2012Article
- Participation of K(ATP) Channels in the Antinociceptive Effect of Pregabalin in Rat Formalin Test.The Korean journal of pain · 2011Article
- Pregabalin modulation of neurotransmitter release is mediated by change in intrinsic activation/inactivation properties of ca(v)2.1 calcium channels.The Journal of pharmacology and experimental therapeutics · 2011Article
- A2delta ligands gabapentin and pregabalin: future implications in daily clinical practice.Hippokratia · 2010Article
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 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundGabapentin and pregabalin have wide-ranging therapeutic actions, and are structurally related to the inhibitory neurotransmitter GABA. Gabapentin, pregablin and GABA can all modulate voltage-activated Ca2+ channels. In this study we have used whole cell patch clamp recording and fura-2 Ca2+ imaging to characterise the actions of pregabalin on the electrophysiological properties of cultured dorsal root ganglion (DRG) neurones from neonatal rats. The aims of this study were to determine whether pregabalin and gabapentin had additive inhibitory effects on high voltage-activated Ca2+ channels, evaluate whether the actions of pregabalin were dependent on GABA receptors and characterise the actions of pregabalin on voltage-activated potassium currents.
resultsPregabalin (25 nM - 2.5 microM) inhibited 20-30% of the high voltage-activated Ca2+ current in cultured DRG neurones. The residual Ca2+ current recorded in the presence of pregabalin was sensitive to the L-type Ca2+ channel modulator, Bay K8644. Saturating concentrations of gabapentin failed to have additive effects when applied with pregabalin, indicating that these two compounds act on the same type(s) of voltage-activated Ca2+ channels but the majority of Ca2+ current was resistant to both drugs. The continual application of GABA, the GABAB receptor antagonist CGP52432, or intracellular photorelease of GTP-gamma-S had no effect on pregabalin-induced inhibition of Ca2+ currents. Although clear inhibition of Ca2+ influx was produced by pregabalin in a population of small neurones, a significant population of larger neurones showed enhanced Ca2+ influx in response to pregabalin. The enhanced Ca2+ influx evoked by pregabalin was mimicked by partial block of K+ conductances with tetraethylammonium. Pregabalin produced biphasic effects on voltage-activated K+ currents, the inhibitory effect of pregabalin was prevented with apamin. The delayed enhancement of K+ currents was attenuated by pertussis toxin and by intracellular application of a (Rp)-analogue of cAMP.
conclusionsPregabalin reduces excitatory properties of cultured DRG neurones by modulating voltage-activated Ca2+ and K+ channels. The pharmacological activity of pregabalin is similar but not identical to that of gabapentin. The actions of pregabalin may involve both extracellular and intracellular drug target sites and modulation of a variety of neuronal conductances, by direct interactions, and through intracellular signalling involving protein kinase A.
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.