Buspirone and related compounds as alternative anxiolytics

  title={Buspirone and related compounds as alternative anxiolytics},
  author={Duncan P. Taylor and S. Moon},
The desire of the pharmaceutical industry to obtain more selective agents for the treatment of anxiety with fewer or diminished side effects and a profile consistent with safety during long-term use resulted in a search which has identified the azapirones as a new class of anxiolytics which lack structural or biochemical homology with the benzodiazepines. This presentation reviews the efficacy of buspirone (BuSpar), the first of this class to reach wide acceptance, and its analogs, gepirone… Expand
Anxiolytic effects of drugs acting on 5-HT receptor subtypes
Anxiolytic effects have been well documented for the 5-HTIApartial agonist azapirones (e.g. buspirone). Benzodiazcpines (which have indirect serotonergic actions) continue to be more widelyExpand
Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan
The plus-maze profile observed with flesinoxan is very similar to that previously reported for 8-OH-DPAT in the same test but, despite superficial similarities, can be distinguished from that seen with buspirone. Expand
Preclinical pharmacology of B-20991, a 5-HT1A receptor agonist with anxiolytic activity.
The results suggest that B-20991 is a 5-HT1A receptor agonist that exhibits anxiolytic activity that causes a dose-related increase in the social interaction and light/dark box behavioral scores. Expand
Augmentation of antipsychotic drug action by azapirone 5-HT1A receptor partial agonists: a meta-analysis.
5-HT1A partial agonists as adjunctive therapy improved overall psychopathology with a trend to improve positive symptoms in patients with schizophrenia. Expand
Azapirones for the treatment of anxiety – an overview
Anxiety disorders belong to the most common psychiatric diagnosis. Over the years, benzodiazepines were considered the gold standard for pharmacological treatment of anxiety. They are effectiveExpand
Behavioural Effects in Mice of Subchronic Buspirone, Ondansetron and Tianeptine. II. The Elevated Plus-Maze
Results show that subchronic treatment with ondansetron failed to influence the behaviour of mice in the plus-maze, while the limited changes induced by buspirone could not be attributed to anxiety-related processes. Expand
Profile of action of 5-HT3 receptor antagonists, ondansetron and WAY 100289, in the elevated plus-maze test of anxiety of mice
It is suggested that the large within- and between-test variability observed with these compounds may indicate an action on mechanisms other than anxiety, as well as the enigmatic effects of 5-HT3 receptor antagonists in animal models of anxiety. Expand
Behavioural Effects in Mice of Subchronic Buspirone, Ondansetron and Tianeptine. I. Social Interactions
The apparent anxiogenic effect of tianeptine is a novel finding which requires further study, while ondansetron had no effect on the categories of behaviour and failed to induce an anxiolytic-like enhancement of social investigation. Expand
Blockade of the anxiolytic-like action of ipsapirone and buspirone, but not that of 8-OH-DPAT, by adrenalectomy in male rats
Data suggest that adrenocortical secretions play a role in the anxiolytic-like actions of buspirone and ipsapirone, but not in those of 8-OH-DPAT, and that adrenaline may be participating in the action of these compounds on the burying behavior latency. Expand
In vivo drug action of tandospirone at 5-HT1A receptor examined using positron emission tomography and neuroendocrine response
Despite the significant effect on growth hormone and body temperature, a clinical dose of tandospirone had a negligible effect on [11C]WAY 100635 binding, which indicates that the agonist produces a pharmacological effect without measurable occupancy, and a new index other than occupancy will be required for the in vivo evaluation of agonists. Expand


Buspirone, a new approach to the treatment of anxiety
  • Duncan P. Taylor
  • Medicine
  • FASEB journal : official publication of the Federation of American Societies for Experimental Biology
  • 1988
Clinical studies have clearly demonstrated the efficacy of buspirone in the treatment of generalized anxiety disorder without the ancillary pharmacology of earlier anxiolytics, and recognize that action at 5‐HT1a receptors may be a viable approach to the pharmacotherapy of anxiety. Expand
Serotonin Agents in Anxiety
Investigation into Buspirone's mechanism of action revealed a key role for serotonin in the pharmacotherapy of anxiety, and a variety of serotonergic agents are now in preclinical and clinical development as anxiolytic agents, including 5-HT1A partial agonists,5-HT2 antagonists, and 5- HT3 antagonists. Expand
Serotonergic mechanisms in the behavioral effects of buspirone and gepirone
Results from these studies suggest that serotonin agonist-like activity may be an important mechanism in the actions of a clinically proven nonbenzodiazepine anxiolytic (buspirone), and anxIOlytic candidate (gepirone). Expand
5-HT1A receptor-related anxiolytics
The novel anti-anxiety agents buspirone, gepirone and ipsapirone which directly affect the serotonergic system by interacting with the 5- HT 1A subtype of the high affinity 5-HT 1 receptor. Expand
Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites
The primary pharmacological effect of tandospirone appears to be partial agonism at the 5-HT1A receptor, an activity similar to other pyrimidinyl-piperazines which are being developed as novel anxiolytic agents. Expand
Characterization of the putative anxiolytic SM-3997 recognition sites in rat brain.
Results indicate that SM-3997 binds selectively and with high affinity to 5-HT-1A receptors in rat brain and may be an agonist. Expand
Effects of the putative anxiolytic SM-3997 on central monoaminergic systems
The serotonergic effect of SM-3997 was similar to that of buspirone, gepirone and ipsapirone, but the dopaminergic effect was much weaker than that ofBuspirone and the effects of other new nonbenzodiazepine anxiolytic compounds were also compared. Expand
Blockade of potentiated startle responding in rats by 5-hydroxytryptamine1A receptor ligands.
A role for the 5-HT1A binding site in the anti-anxiety effects of buspirone and related compounds over a range of behavioral procedures is supported, as well as a role for 1-[3-Chlorophenyl]piperazine, a non-anxiolytic 5- HT1B/1C agonist, in the potentiation of startle induced by the conditional stimulus. Expand
Autoradiographic localization of (3H) gepirone in the rat brain
Gepirone is an anxiolytic compound active at the 5-HT{sub 1A} receptor site. The purpose of this study was to locate the ({sup 3}H)gepirone in the rat brain and to determine the quantity of gepironeExpand
Pharmacology of the serotonergic anxiolytic tandospirone (SM-3997).