Eksp Klin Farmakol. 1994 Jan-Feb;57(1):5-8.
[The characteristics of the pharmacological action of buspirone]

[Article in Russian]

Dzhagatspanian IA, Asrian AB.

Some aspects of the anxiolytic action of buspirone were investigated by differentiating fear from anxiety. Buspirone showing anxiolytic and antineurotic action in the models of anxiety and conflicting situation was demonstrated to be inactive in the model of fear of falling down from the elevated cross-shaped labyrinth. The antiamnestic effect of buspirone was revealed in the electroshock amnesia model. It is assumed that serotonin receptors are possibly responsible both for the anxiety and for memory processes.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8142866&dopt=Abstract buspirone Buspar




Acta Physiol Hung. 1992;79(2):153-61.
Anxiolytic profile of girisopam and GYKI 52,322 (EGIS 6775). Comparison with chlordiazepoxide and buspirone.

Horvath K, Andrasi F, Botka P, Hamori T.

Institute for Drug Research, Budapest, Hungary.

The anxiolytic action of two 2,3-benzodiazepines: girisopam: GYKI 51,189 (EGIS 5810): (1-(3-chlorophenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine), and GYKI 52,322 (EGIS 6775): (1-(4-aminophenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine) was investigated in comparison to chlordiazepoxide and buspirone using three different animal models of anxiety: the lick conflict, the elevated plus maze and the open field methods in rats. Both 2,3-benzodiazepines exerted anxiolytic effect in all three tests used, however their pharmacological profile differs considerably from that of either chlordiazepoxide or buspirone. Using the animal models mentioned above the order of potency was GYKI 52,322 (EGIS 6775) > chlordiazepoxide > girisopam > buspirone.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1363928&dopt=Abstract buspirone Buspar




Braz J Med Biol Res. 1993;26(1):71-4.
Effects of a single administration of buspirone on catalepsy, yawning and stereotypy in rats.

Conceicao IM, Frussa-Filho R.

Departamento de Farmacologia, Escola Paulista de Medicina, Sao Paulo, Brasil.

In the present study, the effects of a single administration of buspirone (0.1, 0.3, 1.0, and 3.0 mg/kg sc-30 min before testing) on three dopamine-related behaviors were evaluated in 4-month old male Wistar rats (7-10 animals per group). Buspirone decreased haloperidol (2.0 mg/kg ip)-induced catalepsy in a dose-dependent manner (from 7.30 to 5.09 1n of s compared to the untreated control group). Apomorphine (0.06 mg/kg sc)-induced yawning was also dose-dependently reduced (from 26.7 to 0.9 yawns in 30 min) and so was apomorphine (1.0 mg/kg sc)-induced stereotypy (from 32.9 to 5.9, sum of scores). The present results indicate that buspirone presents unique pharmacological effects related to dopaminergic transmission not only in biochemical but also in behavioral terms.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8220270&dopt=Abstract buspirone Buspar




Naunyn Schmiedebergs Arch Pharmacol. 1993 Aug;348(2):158-63.
Use-dependent effects of acute and chronic treatment with imipramine and buspirone on excitatory synaptic transmission in the rat hippocampus in vivo.

O'Connor JJ, Rowan MJ, Anwyl R.

Department of Pharmacology and Therapeutics, University of Dublin, Trinity College, Ireland.

The effects of acute and long-term treatment with imipramine and buspirone on the responses of rat hippocampal neurones to low and high frequency electrical stimulation were compared. Whereas acute treatment with imipramine (10 mg/kg, i.p.) had no effect on synaptic responses to low frequency stimulation, chronic treatment for 14 days significantly reduced the amplitude of the field excitatory postsynaptic potential. Both acute and chronic imipramine treatment markedly reduced the amplitude of the nerve volley and excitatory postsynaptic potential evoked at high frequency stimulation rates in a use-dependent manner. Buspirone (0.5-3 mg/kg, i.p.) produced a significant reduction of the excitatory postsynaptic potential at high frequencies. This was enhanced after repeated administration of a dose of 0.5 mg/kg for 14 days. We previously reported a similar effect of buspirone at low frequency stimulation. Both compounds therefore share the ability to exert strong depressant effects on transmission in the hippocampus especially after chronic treatment.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8232595&dopt=Abstract buspirone Buspar




Arzneimittelforschung. 1993 Sep;43(9):942-5.
Suppression of opiate withdrawal and cocaine hyperarousal syndromes by buspirone. Possible pharmacotherapeutic applications.

Aceto MD, Bowman ER.

Department of Pharmacology and Toxicology, Medical College of Virginia, Virginia Commonwealth University, Richmond.

Buspirone (CAS 36505-84-7) was evaluated in three animal models which were designed to study stages of drug abuse most likely associated with compulsive abuse. Buspirone attenuated abrupt withdrawal in rhesus monkeys maximally-dependent on morphine. In addition, it completely blocked the emergence of cocaine-induced stereotyped behavior in rats and attenuated the hyperarousal or rausch syndrome in morphine-dependent and non-dependent rhesus monkeys. Buspirone was active at doses which caused little, if any, impairment in the animals. The results suggest that buspirone may possibly find application in the pharmacotherapy of opioid and cocaine abuse.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8240454&dopt=Abstract buspirone Buspar




Psychiatr Pol. 1993 Sep-Oct;27(5):545-61.
[Buspirone in the treatment of Generalized Anxiety Disorders]

[Article in Polish]

Rzewuska M, Sobucka K.

Samodzielnej Pracowni Farmakoterapii, Instytutu Psychiatrii i Neurologii, Warszawie.

A group of 86 patients, diagnosed with GAD, were treated with doses of 25 mg of Buspirone or 20 mg of Diazepam in a blind study. Comparative efficacy of both drugs and placebo was conducted on 40 patients (archival data). Greater efficacy of Diazepam and Buspirone in states of chronic anxiety was indicated. There were no differences in the intensity of efficacy of both drugs. The effects of Buspirone were equally strong but more general on psychic and somatic anxiety, with the exception of sleep disturbance, in comparison with Diazepam. The efficacy of Buspirone increased after 2 weeks of application. No serious or intensified adverse effects were observed. The incidence of adverse effects was slightly higher in the Buspirone group, and included dizziness, weakness and disturbance of sleep. There were no significant changes in physical examination or laboratory measures.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8255947&dopt=Abstract buspirone Buspar




Pharmacology. 1994 Jan;48(1):1-10.
5-HT1A receptors mediate the effect of the bulbospinal serotonin system on spinal dorsal horn nociceptive neurons.

Zemlan FP, Murphy AZ, Behbehani MM.

Department of Psychiatry, University of Cincinnati College of Medicine, Ohio 45267-0559.

The present study examined whether the effect of stimulation of the nucleus raphe magnus (NRM) is mediated by spinal cord dorsal horn serotonin1A (5-HT1A) receptors in the rat. This hypothesis predicts that nociceptive dorsal horn units inhibited by NRM stimulation or iontophoretic 5-HT application would also be inhibited by iontophoresis of the selective 5-HT1A agonists 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and buspirone. A total of 78 dorsal horn wide-dynamic-range neurons were recorded. Overall, 62% of the cells tested (48/78) were responsive to electrical stimulation of the NRM with the predominant response being inhibitory (38/48; 79%). Fifty-eight cells were tested for their response to both NRM stimulation and 8-OH-DPAT iontophoresis: 20/58 cells were inhibited by NRM stimulation and 50% of the cells inhibited by NRM stimulation were also inhibited by 8-OH-DPAT. Fifty-two cells were tested for their response to both NRM stimulation and buspirone iontophoresis: 14/52 cells were inhibited by NRM stimulation with 9/14 similarly inhibited by buspirone. To examine whether exogenously applied serotonin produced an effect through 5-HT1A receptors, the effect of both 5-HT and 8-OH-DPAT iontophoresis was tested on 57 dorsal horn neurons. The majority of cells (25/57) were inhibited by 5-HT application; 15/25 were similarly inhibited by 8-OH-DPAT. The response of 48 dorsal horn cells to 5-HT and buspirone iontophoresis was compared. Forty-four percent (21/48) of the cells were inhibited by 5-HT; 16/21 were also inhibited by buspirone.(ABSTRACT TRUNCATED AT 250 WORDS)

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8309982&dopt=Abstract buspirone Buspar




Arq Bras Cardiol. 1993 Apr;60(4):269-72.
[Efficacy of and tolerance to buspirone hydrochloride in the treatment of psychosomatic symptoms in clinical cardiology]

[Article in Portuguese]

Ramires JA, Solimene MC, Serrano Junior CV, Mansur Ade P, Pileggi F.

Instituto do Coracao do Hospital das Clinicas, FMUSP.

PURPOSE--To evaluate the efficacy of buspirone hydrochloride in patients of the cardiologic clinic with generalized anxiety. METHODS--Fifty out-patients with psychosomatic cardiovascular symptoms in cardiology were treated for six weeks with initial dose of 5mg of buspirone hydrochloride t.i.d. RESULTS--The results obtained were good in 76% of the patients, fair in 18% and ineffective in 6% of the cases. Thirteen patients (26%) reported at least one adverse event, the side effects reported were: somnolence, headache, flatulence, tinnitus, nasal congestion and dry mouth. No interruption of the treatment was needed. CONCLUSION--Buspirone hydrochloride is a valid alternative for treating pathological anxiety in patients in which the state of alertness and good psychomotor skills must be preserved.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8311738&dopt=Abstract buspirone Buspar