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)

Buspirone and other drugs that act as 5-HT1A agonists appear to be clinically effective anxiolytics in humans, yet their anticonflict effects, though robust in pigeons, are equivocal in rodents. In the present study we examined the effects of the benzodiazepine midazolam and a series of 5-HT1A agonists on punished responding of squirrel monkeys. Lever presses were reinforced according to a fixed-interval 3-min schedule; in addition, each thirtieth lever press was punished. Midazolam produced large increases in response rates, whereas none of the 5-HT1A compounds produced any increases in responding. Most of these drugs decreased response rates at the higher doses examined. Although the reasons for the discrepancy between species in the anticonflict effects of serotonergic anxiolytics cannot be specified, the different anatomical distribution of 5-HT1A binding sites across species may suggest a different functional role for this receptor.
 ...
PMID:5-HT1A agonist effects on punished responding of squirrel monkeys. 198 37

The effect of acute and chronic administration of the 5-HT1A agonist buspirone on successive negative contrast was investigated in Experiments 1-6. Contrast in consummatory behavior was induced by shifting rats from a 32% to a 4% sucrose solution. Experiments 1-5 showed that buspirone (0.125, 0.25, 0.5, 1.0, 2.0, 15.0 mg/kg) was ineffective in alleviating contrast or in facilitating recovery from contrast. The 15 mg/kg dose substantially decreased consummatory responding. Experiment 6 showed that the chronic (24 days) administration of buspirone (0.5, 2.0 mg/kg) also did not alleviate contrast. The chronic, but not the acute administration of the 2.0 mg/kg dose decreased consummatory behavior. In Experiment 7 the 5-HT1A agonist gepirone (2.5, 5.0 and 10.0 mg/kg) was also found to be ineffective in reducing contrast but, at the higher doses, decreased overall sucrose intake. Experiments 8 and 9 found that the 5-HT2 antagonists ketanserin (2.0 and 8.0 mg/kg) and ritanserin (0.63 and 2.5 mg/kg) also did not alleviate contrast. Midazolam (1.0 mg/kg), included as a positive control, eliminated contrast. These data suggest that serotonergic mechanisms are not involved in negative contrast.
 ...
PMID:Effect of serotonergic drugs on negative contrast in consummatory behavior. 214 92

Male rats were adapted to a 22 hr water-deprivation schedule, and to a 30 min test of hypertonic (1.8 or 2.7%) NaCl solution ingestion. A novel benzodiazepine, Ro23-0364, recently reported to have anxiolytic activity in rats and squirrel monkeys but to have limited potential to produce unwanted side effects, produced significant dose-related increases in hypertonic saline ingestion. Midazolam, a benzodiazepine full agonist, increased salt intake but the effect was offset at higher doses by the induction of sedation. Three putative 5-HT1A agonists, proposed as nonbenzodiazepine-related anxiolytics, were also tested: the highly selective 8-OH-DPAT, gepirone and ipsapirone (TVX Q 7821). In each case, occasions when hypertonic saline consumption was significantly increased were detected. At 300 micrograms/kg of 8-OH-DPAT and 10 mg/kg of gepirone, the appearance of a pronounced flattened body posture effectively interfered with drinking responses. It appears possible that a behavioural action shared by benzodiazepines and 5-HT1A agonists may be responsible for the increased hypertonic saline ingestion.
 ...
PMID:Benzodiazepines and putative 5-HT1A agonists increase hypertonic saline consumption in rehydrating rats. 282 18

An involvement of serotonergic innervation of the hippocampus (HP) and the nucleus accumbens septi (NAS) in anxiolytic activity of benzodiazepine midazolam and 5-HT1A receptor agonists was studied in two different animal models of anxiety. Injection of midazolam (10.0 and 20.0 micrograms) or 8-OH-DPAT (0.5 and 1.0 micrograms) into the hippocampus increased punished consumption of water in the Vogel conflict test. Buspirone given at 0.1, 0.5 and 1.0 microgram was ineffective in the Vogel test, while at 5.0 micrograms it enhanced shock-induced suppression of drinking. In the open-field test midazolam (0.01 and 0.1 microgram), 8-OH-DPAT (0.1, 0.5 and 1.0 microgram) and buspirone (2.5 and 5.0 micrograms) increased the number of entries into the central part of the open-field and the time spent in the central sector. Depletion of 5-HT had no influence on the anxiolytic-like effect in the open-field test of intrahippocampally-administered 8-OH-DPAT (0.5 microgram), but the drug tended to increase motor activity in lesioned animals. Midazolam and buspirone injected into the NAS did not have an anxiolytic effect in the Vogel test. A small increase in punished drinking was observed after 8-OH-DPAT (1.0 and 2.5 micrograms). Following intra-NAS injection, midazolam, 8-OH-DPAT and buspirone all failed to produce any marked anxiolytic-like effect in the open-field test. It appears that the hippocampus, rather than the NAS, is involved in mediating anxiolytic-like effects of 5-HT1A receptor agonists. Hippocampal postsynaptic 5-HT1A receptors may account for the anti-emotional influence of this group of drugs. The results indicate some similarities in the psychotropic profile of 5-HT1A receptor agonists and midazolam.
 ...
PMID:Serotonergic innervation of the hippocampus and nucleus accumbens septi and the anxiolytic-like action of midazolam and 5-HT1A receptor agonists. 790 94