Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2007-1-29
pubmed:abstractText
In vivo electrophysiology and microdialysis were used to investigate the physiological role of 5-HT(2C) receptors in the control of substantia nigra pars reticulata (SNr) function. Extracellular single-unit recordings were performed from putative GABA-containing neurons in the SNr of anesthetized rats, and local GABA release was studied by in vivo microdialysis in the SNr of awake freely-moving rats. Systemic administration of the selective 5-HT(2C) receptor agonist (S)-2-(chloro-5-fluoro-indol-1-yl)-1-methylethylamine 1:1 C(4)H(4)O(4) (RO 60-0175) caused a dose-dependent excitation of about 30% of the SNr neurons recorded. However, the remaining neurons were either inhibited or unaffected by systemic RO 60-0175, in similar proportion. Local application of RO 60-0175 by microiontophoresis caused excitation in the majority of SNr neurons tested (48%), whereas a group of neurons was inhibited (16%) or unaffected (36%). Both the excitatory and the inhibitory effects of systemic and microiontophoretic RO 60-0175 were completely prevented by pretreatment with SB 243213 [5-methyl-1-({2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl}carbamoyl)-6-trifluoromethylindoline], a selective and potent 5-HT(2C) receptor antagonist. Consistent with these electrophysiological data, both systemic and intranigral administration of RO 60-0175 and m-chlorophenylpiperazine (mCPP), a non-selective 5-HT(2C) agonist, markedly increased extracellular GABA levels in the SNr. The stimulatory effect of systemic and local RO 60-0175 on GABA release was completely prevented by systemic administration of SB 243213, whereas local application of SB 243213 into the SNr only partially blocked RO 60-0175-induced GABA release. It is concluded that selective activation of 5-HT(2C) receptors stimulates GABA-ergic function in the SNr, and the clinical relevance of these data is discussed.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0306-4522
pubmed:author
pubmed:issnType
Print
pubmed:day
23
pubmed:volume
144
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1523-35
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed-meshheading:17161544-Action Potentials, pubmed-meshheading:17161544-Animals, pubmed-meshheading:17161544-Dose-Response Relationship, Drug, pubmed-meshheading:17161544-Drug Interactions, pubmed-meshheading:17161544-Electrophysiology, pubmed-meshheading:17161544-Excitatory Postsynaptic Potentials, pubmed-meshheading:17161544-Extracellular Fluid, pubmed-meshheading:17161544-Male, pubmed-meshheading:17161544-Microdialysis, pubmed-meshheading:17161544-Neural Inhibition, pubmed-meshheading:17161544-Neurons, pubmed-meshheading:17161544-Rats, pubmed-meshheading:17161544-Rats, Sprague-Dawley, pubmed-meshheading:17161544-Receptor, Serotonin, 5-HT2C, pubmed-meshheading:17161544-Serotonin, pubmed-meshheading:17161544-Serotonin 5-HT2 Receptor Agonists, pubmed-meshheading:17161544-Serotonin 5-HT2 Receptor Antagonists, pubmed-meshheading:17161544-Serotonin Antagonists, pubmed-meshheading:17161544-Serotonin Receptor Agonists, pubmed-meshheading:17161544-Substantia Nigra, pubmed-meshheading:17161544-Synaptic Transmission, pubmed-meshheading:17161544-Up-Regulation, pubmed-meshheading:17161544-gamma-Aminobutyric Acid
pubmed:year
2007
pubmed:articleTitle
Selective activation of 5-HT(2C) receptors stimulates GABA-ergic function in the rat substantia nigra pars reticulata: a combined in vivo electrophysiological and neurochemical study.
pubmed:affiliation
Istituto di Ricerche Farmacologiche "Mario Negri," via Eritera 62, 20157 Milan, Italy.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't