"Ipsapirone"

, previous work indicates that receptors forming heterodimers demonstrate triplet amino acid homologies. The receptor interface of the 5-HT1A-5-HT2A isoreceptor dimer was shown to contain the LLG and QNA protriplets in the transmembrane and intracellular domain, respectively. The 5-HT2A agonist TCB2 markedly reduced the affinity of the 5-HT1A agonist ipsapirone for the 5-HT1A agonist binding sites

an anxiety disorder diagnosis, iii) subject with anxiety as a specifier of another psychiatric condition and not primarily diagnosed.Intervention(s), exposure(s)Inclusion criteria: i) any azapirone (e.g., alnespirone, binospirone, buspirone, enilospirone, eptaspirone, gepirone, ipsapirone, revospirone, tandospirone, zalospirone), ii) any route of administration (e.g., oral, transdermal, others)Exclusion of Bias assessment will be presented in the discussion.Analysis of subgroups or subsetsRegarding efficacy analyses, we will perform subgroup analyses, considering different molecules (e.g., alnespirone, binospirone, buspirone, enilospirone, eptaspirone, gepirone, ipsapirone, revospirone, tandospirone, zalospirone), considering different comparators (e.g., SSRI, TCA, single molecules), when

terms were used: “Anti-Anxiety Agents” [Pharmacological Action] OR meprobamate OR chlordiazepoxide OR diazepam OR alprazolam OR midazolam OR buspirone OR ipsapirone OR clonazepam OR estazolam OR lorazepam OR oxazepam OR triazolam AND “two-way avoidance acquisition” OR “two-way active avoidance test” OR “shuttle box avoidance” OR “two-way shuttle box” OR “two-way shuttle avoidance” AND “Rats” OR rattus

populationsIntervention(s), exposure(s)Inclusion criteria: i) azapirones (e.g., alnespirone, binospirone, buspirone, enilospirone, eptaspirone, gepirone, ipsapirone, revospirone, tandospirone, zalospirone)Exclusion criteria: i) non-azapirone drugsComparator(s)/controlInclusion criteria: i) placebo ii) other active pharmacological treatments iii) Therapy as usual for augmentation trialsExclusion criteria: i

5-HT1A receptor responsivity in unipolar depression. Evaluation of ipsapirone-induced ACTH and cortisol secretion in patients and controls. The selective 5-HT1A receptor ligand ipsapirone (IPS) induces corticotropin (ACTH) and cortisol secretion in humans. To explore 5-HT1A receptor-mediated hypothalamic-pituitary-adrenal (HPA) system activation in depression, 24 subjects (12 patients

Subsensitivity of the 5-hydroxytryptamine1A (5-HT1A) receptor-mediated hypothermic response to ipsapirone in unipolar depression. The selective 5-HT1A receptor ligand ipsapirone (IPS) induces hypothermia in humans. To explore 5-HT1A receptor-mediated thermoregulation in depression, 24 subjects (12 patients with unipolar depression and 12 individually matched controls) received 0.3 mg/kg IPS

Ipsapirone: evidence for efficacy in depression. Sixty-five inpatients of a psychosomatic hospital in the Federal Republic of Germany with the diagnosis of anxiety neurosis (n = 31) or neurotic depression (n = 34) as defined by the International Classification of Disease (ICD-9), were randomized to a 4-week course of ipsapirone at 7.5 mg t.i.d. or placebo in a prospective, double-blind clinical = 34, the intent-to-treat population), the mean change from baseline in the HAM-D at Week 4 (observed cases) was -13.13 +/- 6.06 (n = 16) for the ipsapirone group, and -3.19 +/- 5.99 (n = 16) for the placebo group (p less than .001). A parallel analysis of the change from baseline in the Core Depression score of the HAM-D (defined as the sum of items 1, 2, 3, 7, and 8) also showed a significant

Efficacy and safety of a putative anxiolytic agent: ipsapirone. Ipsapirone is an azopirone derivative that selectively interacts with serotonin-1A (5-HT1A) receptors and fails to affect other neurotransmitter receptors. In this study, ipsapirone at 15 mg or 30 mg was compared with diazepam at 15 mg and placebo in a double-blind, random assignment study design in patients with generalized anxiety disorder (GAD). During 4 weeks of treatment, both active drugs were therapeutically superior to placebo, without significant drug vs. drug therapeutic differences. The side-effect profile of ipsapirone at 15 mg was favorable compared to diazepam, but at 30 mg ipsapirone produced significant gastrointestinal disturbances.

) or by a single dose of the 5-HT1A agonist ipsapirone (IPS). A third group exposed to an ambient temperature of 28 degrees C was given placebo (PLAC). All of the three groups were investigated in a climate chamber. In the CT group the density distribution of blood platelet subpopulations was shifted to an increase in less dense platelets that were more sensitive towards aggregation-inducing agents. The mean

The influence of ipsapirone, a 5-HT1A agonist, on sleep patterns of healthy subjects. Ipsapirone is a new pyrimidinylpiperazine ligand specific for 5-HT1A receptors, with potential therapeutic use in affective disorders. Because 5-HT is involved in the regulation of sleep, we investigated the effect of ipsapirone hydrochloride on sleep patterns in 18 normal, healthy subjects of both sexes . Compared to placebo, ipsapirone 5 mg administered by mouth three times daily for 14 days decreased rapid eye movement (REM) sleep duration and, by the tenth day of treatment, began to reduce slow wave sleep (SWS) duration. The decrease in REM sleep occurred in the first 3 h of sleep. The latency to REM sleep was increased from the first night following ipsapirone administration, remained increased

Effects of buspirone on plasma prolactin and cortisol levels in major depressed and normal subjects. The cortisol response to ipsapirone (a 5-HT1A-partial agonist that produces a dose-dependent increase in plasma cortisol secretion in man) is blunted in major depression. Buspirone is another 5-HT1A agonist that increases cortisol secretion in man. This study investigated cortisol and prolactin

A phase II multicenter dose-finding, efficacy and safety trial of ipsapirone in outpatients with generalized anxiety disorder. Benzodiazepines have been prescribed for the treatment of Generalized Anxiety Disorder (GAD) for nearly three decades due to their proven anxiolytic efficacy, despite a considerable side effect and abuse liability profile. A new class of compounds, the azapirones, have been developed as an alternative to benzodiazepine treatment. Ipsapirone is a novel anxiolytic azapirone which has high specificity for the 5-HT1A receptor and which has the potential for offering certain advantages over buspirone. The present 5-week study investigated three doses of ipsapirone (2.5mg, 5.0mg and 7.5mg tid) versus placebo in 267 GAD outpatients. Efficacy was evaluated using

Effects of ipsapirone on plasma cortisol and body temperature in major depression. Major depressed patients have been reported to exhibit significantly attenuated hypothermic responses to ipsapirone, a serotonin (5-HT)-1A partial agonist, compared to normal controls. This study further investigated the cortisol and temperature responses to ipsapirone (0.5 mg/kg orally) and placebo in 20 normal volunteers and 12 major depressed patients. Both plasma cortisol and temperature were measured every 30 min before ipsapirone or placebo administration until 180 min post administration. Ipsapirone administration produced a significant increase in plasma cortisol levels as well as hypothermia. Major depressed patients showed significantly blunted ipsapirone-induced cortisol responses compared to normal

5-HT agonist-induced changes in peripheral immune cells in healthy volunteers: the impact of personality. The present study was conducted to investigate the relationship between the serotonergic neurotransmitter system and migration patterns of peripheral lymphocytes. Altogether 40 healthy male volunteers were given either a single dosage of the 5-HT1a-receptor agonist ipsapirone (10 mg by questionnaires to investigate personality related differences in levels of serotonergic responsiveness. Analyses of covariance indicated that ipsapirone leads to highly significant reductions of peripheral CD4+ cells (T-helper/inducer-cells). This was significantly correlated to the ipsapirone-induced release of cortisol in a time-dependent manner. Furthermore, subjects scoring high on impulsivity

Complex effects of age and gender on hypothermic, adrenocorticotrophic hormone and cortisol responses to ipsapirone challenge in normal subjects. The effects of a challenge dose of the 5-HT1A agonist, ipsapirone (0.3 mg per kg body weight), or placebo on body temperature and on adrenocorticotrophic hormone (ACTH) and cortisol release, were examined in 30 normal subjects (14 males, 19-74 years and 16 females, 22-69 years) using a randomized, double blind design. Irrespective of age or gender, ipsapirone induced a significant reduction in body temperature relative to placebo and a significant increase in ACTH and cortisol release. Maximal temperature reduction by ipsapirone was significantly blunted in older subjects and was inversely related to age. There was no gender difference

Placebo-controlled comparison of the clinical effects of rapid discontinuation of ipsapirone and lorazepam after 8 weeks of treatment for generalized anxiety disorder. One hundred and sixty patients (mean age 39.8 years; 67% female) diagnosed with generalized anxiety disorder (GAD) who had completed a prospective, 8 week, double-blind comparison of lorazepam (mean daily dose 4.2 mg ) and ipsapirone (mean daily dose 19.5 mg) were rapidly tapered by a substitution of half-strength medication for 3 days, then substitution of matched placebo for an additional 11 days. Patients treated with ipsapirone showed no rebound anxiety on discontinuation, nor any other significant increase in withdrawal symptomatology compared to patients who had been prospectively treated with placebo. In contrast

Effect of pindolol on hormone secretion and body temperature: partial agonist effects. Pindolol has been shown to be a partial agonist at 5-HT1A receptors in preclinical studies. It has also been reported to inhibit the effects of other 5-HT1A partial agonists such as ipsapirone and buspirone on hormone secretion and body temperature in man, indicating its antagonist action at 5-HT1A receptors

Inhibition of REM sleep by ipsapirone, a 5HT1A agonist, in normal volunteers. In order to test the hypothesis that serotonergic mechanisms inhibit REM sleep via a 5HT1A receptor, we administered placebo and ipsapirone (10 and 20 mg by mouth 15 min before bedtime) to ten normal volunteers in a double blind fashion. Ipsapirone is a relatively selective 5HT1A receptor agonist. As predicted , ipsapirone prolonged REM latency and Mean Latency to Eye Movements (M-LEM), a measure of time between onset of REM sleep and the first eye movement of the REM period, and REM% at both doses compared with placebo. It also reduced sleep efficiency and total REM sleep time at the highest dose. These results support the hypothesis that systemic stimulation of 5HT1A receptors prolong REM latency and inhibit REM

Neuroendocrine effects of ipsapirone on the hypothalamic-pituitary adrenal axis: CRF, ACTH and cortisol in healthy volunteers. The neuroendocrine effects (changes in plasma CRF, ACTH and cortisol) of single and multiple (t.d.s. for 2 days) doses of ipsapirone (BAY Q 7821) 5 and 10 mg have been investigated in 6 healthy male volunteers. The study followed a balanced complete block, placebo -controlled and double blind design with two baseline phases (pre and post-treatment). Volunteers were investigated on identical days during 5 successive weeks. The results do not show a specific effect of ipsapirone on the hypothalamic-pituitary-adrenal axis when doses in the range of 5-30 mg per day were given.