PMID: 8584043Sep 1, 1995Paper

BIMT 17, a 5-HT1A receptor agonist/5-HT2A receptor antagonist, directly activates postsynaptic 5-HT inhibitory responses in the rat cerebral cortex

Naunyn-Schmiedeberg's Archives of Pharmacology
Franco BorsiniA Donetti

Abstract

BIMT 17 (1-[2-[4-(3-trifluoromethyl phenyl) piperazin-1-yl] ethyl] benzimidazol- [1H]-2-one), a 5-HT1A receptor agonist/5-HT2A receptor antagonist (see Borsini et al., accompanying paper), in a dose range of 1-10 mg/kg i.v., dose-dependently inhibited the electrical activity of rat medial prefronto-cortical neurons, whereas buspirone, in a dose range of 0.1-1000 micrograms/kg, increased it. 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) and 1-[2-(2-thenoylamino)ethyl]-4-[1-(7-methoxynaphthyl)] piperazine (S 14671) presented biphasic patterns of response; they increased electrical activity at doses in the range of 0.1-10 micrograms/kg and 0.1-3 micrograms/kg i.v. respectively, and reduced it at high doses, 30-300 micrograms/kg and 10-30 micrograms/kg i.v., respectively. The inhibitory effect of BIMT 17 on the firing rate of neurons in the frontal cortex was antagonized by the 5-HT1A antagonists tertatolol and WAY 100135, and was still present after destruction of serotonin (5-HT) containing neuronal endings by the neurotoxin 5,7-dihydroxytryptamine (5,7-DHT; 150 micrograms/rat, given intraventricularly), which reduced the cortical 5-HT content by 85%. This destruction of 5-HT neurons, while suppressing the ability of 8-OH-D...Continue Reading

Citations

Jan 5, 2002·European Journal of Pharmacology·F Borsini, R Cesana
Sep 24, 1999·Pharmacology, Biochemistry, and Behavior·F BorsiniN Pitsikas
Jan 26, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·A BrambillaF Borsini
Jan 22, 2013·ACS Chemical Neuroscience·Stefanie C AltieriAnne M Andrews
Dec 5, 2013·Neuroscience and Biobehavioral Reviews·Ian MaharJosé N Nobrega
Nov 19, 2013·Pharmacology, Biochemistry, and Behavior·Lynda Uphouse
Feb 25, 2014·Neurological Sciences : Official Journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology·Qiaojun ZhangJian Liu
Dec 5, 2015·The Journal of Sexual Medicine·Alexander K ConverseDavid H Abbott
May 21, 2009·The Journal of Sexual Medicine·James G Pfaus
Apr 29, 2008·Neuroscience and Biobehavioral Reviews·Andrew Holmes
Nov 13, 2007·Trends in Pharmacological Sciences·Trevor SharpPhilip Quérée

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