The anticonvulsant, antihyperalgesic agent gabapentin is an agonist at brain γ-aminobutyric acid type B receptors negatively coupled to voltage-dependent calcium channels

Journal of Pharmacology and Experimental Therapeutics

Volumn 298, Issue 1, 2001, Pages 15-24

  Bertrand, Sandrine ^a   Ng, Gordon Y K ^b   Purisai, Maya Gadhvi ^c   Wolfe, Shannyn E ^c   Severidt, Mathew W ^c   Nouel, Dominique ^a   Robitaille, Richard ^a   Low, Malcolm J ^e   O'Neill, Gary P ^b   Metters, Kathleen ^b   Lacaille, Jean Claude ^a   Chronwall, Bibie M ^c   Morris, Stephen J ^d  

^a UNIVERSITÉ DE MONTRÉAL   (Canada)

^b MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

^c UNIVERSITY OF MISSOURI KANSAS CITY   (United States)

^d STOWERS INSTITUTE FOR MEDICAL RESEARCH   (United States)

^e OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR STIMULATING AGENT; BACLOFEN; BENZYL[3 [[1 (3,4 DICHLOROPHENYL)ETHYL]AMINO] 2 HYDROXYPROPYL]PHOSPHINIC ACID; CALCIUM CHANNEL; GABAPENTIN;

ACTION POTENTIAL; ANIMAL CELL; ANIMAL TISSUE; ANTICONVULSANT ACTIVITY; ARTICLE; CONVULSION; DRUG MECHANISM; HIPPOCAMPUS; HYPERALGESIA; MOUSE; NONHUMAN; PRIORITY JOURNAL;

ACETIC ACIDS; AMINES; ANALGESICS; ANIMALS; ANTICONVULSANTS; BACLOFEN; CALCIUM CHANNELS; CALCIUM SIGNALING; CYCLOHEXANECARBOXYLIC ACIDS; GABA AGONISTS; GAMMA-AMINOBUTYRIC ACID; HIPPOCAMPUS; MALE; MICE; MICE, TRANSGENIC; PYRAMIDAL CELLS; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GABA-B;

EID: 0034967810     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Calcium regulation of intracellular pH in pituitary intermediate lobe melanotropes
2. γ-Aminobutyric acid type B receptor splice variant proteins GBR1a and GBR1b are both associated with GBR2 in situ and display differential regional and subcellular distribution
3. B receptor isoforms GBR1a and GBR1b, appear to be associated with pre- and post-synaptic elements respectively in rat and human cerebellum
4. B receptors: First of the functional metabotropic heterodimers
5. 3-Substituted GABA analogs with central nervous system activity: A review
6. B2 genes
7. +-evoked glutamate release from rat neocortical and hippocampal slices by gabapentin
8. B receptor-mediated inhibition of GABA release in area CA1 of the rat hippocampus
9. B receptors in NG108-15 cells
10. BR2 receptor subunits inhibits: Calcium current in sympathetic neurons
11. 2+ influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices
12. 2δ subunit of a calcium channel
13. Effects of intrathecally administered THIP, baclofen, and muscimol on nociceptive threshold
14. 2+ channel modulation in rat sensory neurones
15. Pharmacological studies of the prolonged depressant effects of baclofen on lumbar dorsal horn units in the cat
16. 2+ channels by G-protein subunits
17. Two distinct pituitary cell lines from mouse intermediate lobe tumors: A cell that produces prolactin-regulating factor and a melanotroph
18. Voltage-dependent modulation of N-type calcium channels by G-protein βγ subunits
19. 2+ currents in rat hippocampal interneurones and their selective inhibition by activation of GABA(B) receptors
20. Effects of intrathecal baclofen on chronic spinal cord injury pain
21. Posttranslational processing of proopiomelanocortin (POMC) in mouse pituitary melanotroph tumors induced by a POMC-simian virus 40 large T antigen transgene
22. A receptor activation, inhibits electrically evoked substance P-like immunoreactivity release from spinal cord in vitro
23. Calcitonin gene-related peptide content, basal outflow and electrically evoked release from monoarthritic rat spinal cord in vitro
24. B-receptor modulation of N-type calcium channels in cultured dorsal root ganglion neurons
25. GABA B R1a/R1b-type receptor antisense deoxynucleotide treatment of melanotropes blocks chronic GABA B receptor inhibition of high voltage activated calcium channels
26. Rapid simultaneous estimation of intracellular calcium and pH
27. γ-Aminobutyric acid type B receptors with specific heterodimer composition and postsynaptic actions in hippocampal neurons are targets of anticonvulsant gabapentin action
28. B synaptic transmission in area CA1 of the Rat hippocampus
29. Gabapentin inhibits excitatory synaptic transmission in the hyperalgesic spinal cord
30. Gabapentin actions on ligand- and voltage-gated responses in cultured rodent neurons
31. D-Baclofen is an antagonist at baclofen receptors mediating antinociception in the spinal cord
32. 2+ currents and synaptic transmission in cultured rat hippocampal neurones
33. Effects of phenytoin, carbamazepine, and gabapentin on calcium channels in hippocampal granule cells from patients with temporal lobe epilepsy
34. Gabapentin affects glutamatergic excitatory neurotransmission in the rat dorsal horn
35. Gabapentin inhibits calcium currents in isolated rat brain neurons
36. 2+]
37. A summary of mechanistic hypotheses of gabapentin pharmacology
38. 2+, exocytosis and endocytosis in single melanotropes of the rat pituitary
39. B receptor protein and mRNA distribution in rat spinal cord and dorsal root ganglia
40. Presynaptic inhibition of elicited neurotransmitter release
41. Gabapentin has an antinociceptive effect mediated via a spinal site of action in a rat model of painful peripheral neuropathy