Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P08908 (5-HT1A)
 5,574 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects of spiroxatrine, a putative antagonist with selectivity for the serotonin (5-HT)1A receptor, were compared with compounds believed to function as agonists at the 5-HT1A receptor. Schedule-controlled responding of pigeons was maintained under a multiple 30-response fixed-ratio (FR), 3-min fixed-interval (FI) schedule or under a schedule in which responding was suppressed by electric shock ("conflict" procedure). Under the multiple schedule, spiroxatrine (0.3-1.0 mg/kg) decreased FR responding but did not affect FI responding; responding was decreased in both schedule components at 3.0 mg/kg. When administered alone, buspirone, a compound believed to produce its anxiolytic effects through 5-HT1A agonist actions, produced effects similar to those of spiroxatrine; in combination, the two drugs produced greater effects than when either was administered alone. As with 5-HT1A agonists such as buspirone and 8-hydroxy-2(di-n-propylamino)tetralin (8-OH-DPAT) in the pigeon, spiroxatrine (0.01-1.0 mg/kg) increased punished responding. Spiroxatrine and buspirone were potent inhibitors of [3H]8-OH-DPAT binding to pigeon cerebral membranes with IC50 values in the nM range. Neurochemical analyses of metabolite changes produced by spiroxatrine in pigeon cerebrospinal fluid showed buspirone-like effects, with increases in MHPG, DOPAC and HVA at doses that decreased 5-HIAA levels. Spiroxatrine dose-dependently blocked the behavioral effects of the dopamine agonist piribedil indicating that, like buspirone, it also is a potent dopamine antagonist. Spiroxatrine most likely functions as an agonist at the 5-HT1A receptor. As with buspirone, however, spiroxatrine has a prominent dopamine antagonist component.
 ...
PMID:Behavioral and neurochemical effects of the serotonin (5-HT)1A receptor ligand spiroxatrine. 252 83

The effects of R(+)-8-hydroxy-dipropylaminotetralin (8-OHDPAT) administration into the dorsal raphe nucleus (DRN) or bilaterally into the dorsal hippocampus (HIP) on fear behavior in a modified version of the light-dark transitions test and regional brain monoamines (NA, DA, 5-HT) and their metabolites (MHPG, DOPAC, 5-HIAA) in the hypothalamus, midbrain central gray matter, amygdala, hippocampus and pons were examined. The experiments were performed on 36 male, 3-month old Wistar rats. Administration of 8-OHDPAT (200 ng) into the DRN reduced time out from the illuminated part of the chamber and time of motionless behavior in the illuminated part, increased the number of returns from the dark to illuminated part and number of head dipping from the dark to illuminated part without effect on time of motionless behavior in the dark part and on time of locomotor activity in the illuminated as well as in dark part of the chamber. HPLC analysis showed reduction of 5-HT content in the midbrain and amygdala, reduction of 5-HIAA content in pons, increased 5-HIAA/5-HT ratio in the hippocampus and increased DOPAC/DA ratio in the hypothalamus, midbrain, hippocampus and pons without affecting the MHPG/NA ratio and NA content. The administration of 8-OHDPAT (100 ng per site) into the HIP reduced time out from the illuminated part of chamber, time of locomotor activity in the illuminated part and head dipping from the dark to illuminated part without effect on the number of returns from the dark to illuminated part, time of locomotor activity in the dark part and time of motionless in the illuminated as well as in the dark part of chamber. HPLC analysis showed reduction of NA content in the hypothalamus, amygdala and pons, increased the MHPG content in all the investigated structures, increased MHPG/NA ratio in all the investigated structures except the hypothalamus. Dopamine content decreased in the hypothalamus and amygdala, and DOPAC/DA ratio increased in the amygdala and hippocampus. Concentrations of 5-HT, 5-HIAA and 5-HIAA/5-HT ratio were unchanged. The results obtained indicate that 8-OHDPAT acting on the pre-synaptic 5-HT1A receptors decreases fear behavior and acting on 5-HT1A post-synaptic receptors increases fear behavior in the light-dark transitions test. The neurochemical base of anxiolytic and anxiogenic effects evoked by 8-OHDPAT is being discussed.
 ...
PMID:Effects of 8-OHDPAT administration into the dorsal raphe nucleus and dorsal hippocampus on fear behavior and regional brain monoamines distribution in rats. 1117 84

The effects of 8-OHDPAT and UH-301 injection into the dorsal raphe nucleus (DRN) on fear behavior of the light-dark transitions test and regional brain monoamines (NA, DA, 5-HT) and their metabolites (MHPG, DOPAC, 5-HIAA) in the hypothalamus (HPT), midbrain central gray matter (MID), amygdala (AMY), hippocampus (HIP) and pons (PO) were examined. An injection of 8-OHDPAT (300 ng) as well UH-301 (300 ng) into the DRN evoked an increase in the number of head dipping from dark to the illuminated compartment of chamber, an increase of time of motionless in the dark compartment and decrease of time of locomotion activity in the illuminated compartment. HPLC analysis showed reduction of 5-HIAA/5-HT ratio in the HPT, HIP and PO, increase of MHPG/NA ratio in the HIP and PO, and increase of DA content in the HPT, AMY and HIP after 8-OHDPAT injection. But injection of UH-301 reduced 5-HT in the MID and increased in the AMY, reduced 5-HIAA content in the HIP and increased in the MID and decreased MHPG/NA ratio in the PO. These results indicate that both 5-HT1A receptor agonists, acting on the 5HT1A autoreceptors caused the anxiolytic effects, reduced fear behavior on the rat connected with infringement of dynamic balance between the serotonergic and catecholaminergics systems.
 ...
PMID:Fear behavior and regional brain monoamines distribution after R(+)-8-OHDPAT and R(+)-UH-301 injections into the dorsal raphe nucleus in rats. 1220 Oct 34