Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1994-3-18
pubmed:abstractText
SR 57746A (1-[2-(naphth-2-yl) ethyl]-4-(3-trifluoromethylphenyl)-1, 2, 5, 6 tetra-hydropyridine hydrochloride) binds competitively, and with high affinity (Ki = 2.0 +/- 0.7 nM) to 5-HT1A receptors from rat hippocampus in vitro, but has much less affinity for other 5-HT receptor subtypes (IC50 > 650 nM). SR 57746A produces a concentration-dependent inhibition of forskolin-stimulated adenylate cyclase activity in rat hippocampal homogenates, with a maximal effect identical to that of 8-OH-DPAT, suggesting that SR 57746A behaves as a full agonist in this experimental model. SR 57746A potently displaces [3H]8-OH-DPAT binding to rat hippocampal membranes ex vivo, with an ID50 of 11.1 mg/kg po, 30 min after administration, and 2.8 mg/kg po, 2 h after administration. This effect of SR 57746A is long-lasting (at least 24 hours at 10 mg/kg po). SR 57746A does not modify the levels of 5-HT or DA in various brain areas, but decreases the concentrations of 5-HIAA, and increases those of DOPAC, HVA and 3-MT. Following i.v. administration, SR 57746A (0.095 to 0.25 mg/kg) inhibits the spontaneous firing of dorsal raphe neurones, but does not modify the activity of DA neurones in the substantia nigra or ventral tegmental area. Thus, SR 57746A is a potent, selective and full agonist at 5-HT1A receptors in vitro and vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0767-3981
pubmed:author
pubmed:issnType
Print
pubmed:volume
7
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
487-97
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed-meshheading:8314196-8-Hydroxy-2-(di-n-propylamino)tetralin, pubmed-meshheading:8314196-Adenylate Cyclase, pubmed-meshheading:8314196-Amines, pubmed-meshheading:8314196-Animals, pubmed-meshheading:8314196-Electrophysiology, pubmed-meshheading:8314196-Hippocampus, pubmed-meshheading:8314196-Male, pubmed-meshheading:8314196-Membranes, pubmed-meshheading:8314196-Naphthalenes, pubmed-meshheading:8314196-Neurons, pubmed-meshheading:8314196-Pyridines, pubmed-meshheading:8314196-Raphe Nuclei, pubmed-meshheading:8314196-Rats, pubmed-meshheading:8314196-Rats, Sprague-Dawley, pubmed-meshheading:8314196-Receptors, Serotonin, pubmed-meshheading:8314196-Serotonin Receptor Agonists, pubmed-meshheading:8314196-Substantia Nigra, pubmed-meshheading:8314196-Tritium, pubmed-meshheading:8314196-Ventral Tegmental Area
pubmed:year
1993
pubmed:articleTitle
Biochemical and electrophysiological properties of SR 57746A, a new, potent 5-HT1A receptor agonist.
pubmed:affiliation
Sanofi Recherche, Toulouse, France.
pubmed:publicationType
Journal Article, Comparative Study