Exxua (gepirone)
Research Synopsis
- Recent studies have shown that Exxua (gepirone) displays significant anxiolytic effects, as evidenced by a pilot study in which its use significantly reduced anxiety scores in patients with generalized anxiety disorder.
- Gepirone treatment for 28 days resulted in a notable decrease in serotonin type 2 (5HT2) receptor density, indicating its potential influence on serotonin systems relevant to anxiety and depression.
- The compound has been reported to enhance serotonergic and dopaminergic actions in various animal models, which might contribute to its therapeutic efficacy.
- Gepirone's metabolites, particularly 1-(2-pyrimidinyl)-piperazine (PmP), show prolonged effects and involvement in its anxiolytic actions, signaling their importance in understanding gepirone's mechanism of action.
- Notably, gepirone has been shown to selectively reduce aggressive behavior in animal models, further supporting its potential use in anxiety treatment without sedative effects.
- The pharmacological profile of gepirone indicates weak affinity for certain adrenergic receptors, suggesting a complex interplay of neurotransmitter systems involved in its anxiolytic effects.
- Research findings emphasize the need for further studies to elucidate gepirone's distinct serotonergic receptor interactions, which differentiate it from traditional benzodiazepines.
- Gepirone's polymorphic forms, which influence its pharmacological properties, highlight the importance of formulation stability in utilizing this compound for therapeutic purposes.
- Overall, gepirone is positioned as a promising candidate in the non-benzodiazepine anxiolytic landscape, meriting additional clinical investigation for its safety profile and efficacy.
- Further understanding of gepirone’s unique mechanisms can aid in developing optimized anxiolytic therapies.
Exxua (gepirone)
Comparative neuropharmacology of buspirone and MJ-13805, a potential anti-anxiety drug.
London, UK
2 hours ago
1 Received
- Buspirone is an effective anti-anxiety medication that doesn't have the typical effects associated with benzodiazepines, unlike its analog MJ-13805.
- Both buspirone and MJ-13805 affect dopaminergic systems, with buspirone increasing dopamine metabolism, while MJ-13805 does not significantly impact dopamine autoreceptors.
- The findings suggest that buspirone may work through different mechanisms for its anti-anxiety effects and its ability to reverse catalepsy, potentially making it a candidate for testing in movement disorder treatments.
$100 - $150
Hourly Rate
The effects of buspirone, BMY-13805 and 1-(2-pyrimidinyl)-piperazine on cat spinal reflexes.
London, UK
2 hours ago
1 Received
- * In an intact neuraxis setup, buspirone produced significant changes in spinal reflexes, characterized by a bimodal response: an initial change within 1 hour, followed by a decrease, and then another significant alteration after 3 hours.
- * The observed changes included increased dorsal root potential and modifications in the conditioned monosynaptic reflex, suggesting that buspirone influences higher brain mechanisms rather than directly affecting spinal reflexes.
$100 - $150
Hourly Rate
Reduction in cortical 5HT2 receptor sensitivity after continuous gepirone treatment.
London, UK
2 hours ago
1 Received
- Continuous treatment with gepirone for 28 days led to a 17% decrease in serotonin type 2 (5HT2) receptor density in rat cortical areas.
- Gepirone also reduced head shakes caused by the serotonin agonist quipazine, indicating its influence on serotonin-related behavior.
- These findings align with earlier research, suggesting gepirone may act as an anxiolytic and share properties typically seen in effective antidepressants.
$100 - $150
Hourly Rate
Disposition of the psychotropic drugs buspirone, MJ-13805 and piribedil, and of their common active metabolite 1-(2-pyrimidinyl)-piperazine in the rat.
London, UK
2 hours ago
1 Received
- 1-(2-Pyrimidinyl)-piperazine (PmP) is a metabolite formed from the drugs buspirone, MJ-13805, and piribedil, and it has a longer half-life than its parent drugs.* -
- After intravenous injection in rats, the parent drugs are quickly cleared from the body, while PmP remains for a more extended period.* -
- PmP is significantly concentrated in the brain, suggesting its formation plays an important role for buspirone and MJ-13805, but is less significant for piribedil.*
$100 - $150
Hourly Rate
Characterization of polymorphism of gepirone hydrochloride.
London, UK
2 hours ago
1 Received
- Gepirone hydrochloride, an investigational drug for anxiety, has three polymorphic forms with different melting points: 180°C (I), 212°C (II), and 200°C (III).
- Thermal analysis revealed that forms I and II are enantiotropic, meaning they can convert into each other, while form III is monotropic, only stable relative to form II.
- Form I is more stable at temperatures below 74°C, while form II is more stable above that point; techniques like hot-stage microscopy helped identify the presence of these forms in samples.
$100 - $150
Hourly Rate
Monoaminergic involvement in the pharmacological actions of buspirone.
London, UK
2 hours ago
1 Received
- - Buspirone, MJ-13805, and MJ-13653 were tested in rats and did not cause '5-HT syndrome' even at high doses (up to 20 mg kg-1) and are weak serotonin uptake blockers.
- - These drugs do not inhibit monoamine oxidase types A or B, indicating a different mechanism compared to stronger antidepressants like chlorimipramine.
- - Buspirone did show effects in controlling certain behaviors, such as blocking stereotypy induced by apomorphine and delaying effects from other serotonin-related compounds.
$100 - $150
Hourly Rate
Serotonergic mechanisms in the behavioral effects of buspirone and gepirone.
London, UK
2 hours ago
1 Received
- * Both drugs show effects in anxiety-related behaviors that are influenced by serotonin levels, as indicated by changes in behavior when serotonin is disrupted in studies.
- * Results imply that serotonin agonist-like activity could be key for the effectiveness of buspirone, a clinically approved anxiolytic, and gepirone, an emerging candidate.
$100 - $150
Hourly Rate
A study of the effects of buspirone, BMY 13805, and 1-PP on dopaminergic metabolism in the nucleus accumbens using in vivo voltammetry in freely moving rats.
London, UK
2 hours ago
1 Received
- The study examined how buspirone, its analogue BMY 13805, and its metabolite 1-PP affect dopamine levels in the nucleus accumbens using advanced measurement techniques.
- Results showed that buspirone significantly increased DOPAC levels in this brain region, with subcutaneous injections being ten times more effective than intraperitoneal ones.
- However, BMY 13805 and 1-PP did not influence dopaminergic metabolism, suggesting that the anxiety-reducing effects of these substances are not linked to changes in dopamine levels.
$100 - $150
Hourly Rate
Behavioral studies with anxiolytic drugs. III. Antipunishment actions of buspirone in the pigeon do not involve benzodiazepine receptor mechanisms.
London, UK
2 hours ago
1 Received
- Buspirone is an effective anxiolytic that shows inconsistent antianxiety effects in traditional animal tests but significantly increases punished responding in pigeons under a conflict procedure.
- The buspirone analog MJ 13805 produced similar results to buspirone, although it slightly affected unpunished responding more than buspirone did.
- None of the tested compounds, including a metabolite of buspirone, impacted [3H]diazepam binding in pigeon brains, indicating that the effects of buspirone are not linked to the benzodiazepine receptor complex.
$100 - $150
Hourly Rate
[Effect of anxiolytics--buspirone and diazepam--on the prolactin, thyrotropin and cortisol content of the blood in the green monkey].
London, UK
2 hours ago
1 Received
- The study examined how the anxiolytics diazepam and buspirone affect hormone levels in green monkeys, specifically prolactin, thyrotrophin, and cortisol, after an intramuscular injection.
- Diazepam (1 mg/kg) significantly lowered prolactin and cortisol levels by 30-50% compared to controls, suggesting a calming effect on these hormones.
- In contrast, buspirone (2.5-10 mg/kg) caused a dramatic increase in prolactin levels (7-10 times higher) without affecting cortisol or thyrotrophin, while a related compound, Mj 138-05, had varied effects on prolactin depending on the dose.
$100 - $150
Hourly Rate
Effects of 5-HT1A selective anxiolytics on lordosis behavior: interactions with progesterone.
London, UK
2 hours ago
1 Received
- Ipsapirone and gepirone enhanced lordosis behavior in estrogen-treated rats, while buspirone did not have this effect.
- All three drugs suppressed lordosis in rats treated with both estrogen and progesterone, especially at higher doses.
- The findings support the idea that 5-HT1A receptors are involved in inhibiting lordosis, and indicate that progesterone may influence how these receptors function.
$100 - $150
Hourly Rate
Pharmacological evidence for the involvement of 1-(2-pyridinyl)-piperazine (1-PmP) in the interaction of buspirone or gepirone with noradrenergic systems.
London, UK
2 hours ago
1 Received
- The study examined how 1-(2-pyridinyl)-piperazine (1-PmP), a metabolite of buspirone and gepirone, affects hypothermia and decreased movement in mice triggered by clonidine, which tests brain alpha-adrenergic functions.
- It was found that 1-PmP can dose-dependently counteract the hypothermia and reduced locomotion caused by clonidine when administered at doses ranging from 1-16 mg/kg.
- Additionally, using proadifen prior to buspirone and gepirone treatment blocked their ability to reverse clonidine's effects on body temperature, indicating that 1-PmP may play a role in the noradrenerg
$100 - $150
Hourly Rate
Gepirone in anxiety: a pilot study.
London, UK
2 hours ago
1 Received
- A study treated ten patients with generalized anxiety disorder using the medication gepirone after a week without any treatment to establish a baseline.
- Over six weeks, the average anxiety scores significantly decreased from 24.8 to 7.1, indicating a strong improvement.
- Gepirone was well tolerated by patients, showed no sedative effects, and demonstrated promising anxiolytic effects, suggesting potential for future use.
$100 - $150
Hourly Rate
Discriminative stimulus properties of buspirone in the pigeon.
London, UK
2 hours ago
1 Received
- The study investigated the effects of the anxiolytic drug buspirone on pigeons, using a two-key drug discrimination task to identify its stimulus properties and potential anticonflict mechanisms.
- Pigeons were trained to distinguish between buspirone at a dose of 1.0 mg/kg and saline, followed by generalization tests that showed a strong response to buspirone and similar compounds, while other drugs like midazolam and haloperidol did not produce the same response.
- The findings suggest that serotonin receptors, especially 5-hydroxytryptamine-1A receptors, are likely involved in the anxious-reducing effects of buspirone, indicating its action is not primarily through the dopaminergic
$100 - $150
Hourly Rate
Effects of gepirone, an aryl-piperazine anxiolytic drug, on aggressive behavior and brain monoaminergic neurotransmission.
London, UK
2 hours ago
1 Received
- Gepirone, a drug similar to buspirone, was tested for its ability to reduce anxiety in mice, showing effectiveness in inhibiting aggressive behavior without causing sedation.
- The drug's effects were enhanced when paired with methiothepin or methysergide, and it specifically decreased serotonin (5HT) neurotransmission while also affecting dopamine metabolism differently than buspirone.
- Overall, gepirone appears to function primarily by reducing serotonergic activity, which aligns with findings that decreased serotonin can have anxiolytic effects in animal models.
$100 - $150
Hourly Rate
Tissue-dependent alpha adrenoceptor activity of buspirone and related compounds.
London, UK
2 hours ago
1 Received
- The study investigates the binding and effectiveness of buspirone and its related compounds (gepirone, isapirone, and a metabolite) on alpha adrenoceptors, specifically comparing the alpha-1 and alpha-2 subtypes.
- It was found that these compounds have weak affinity for alpha-1 adrenoceptors but show significant intrinsic efficacy that varies by tissue type and species, with buspirone being the most effective among them.
- No intrinsic efficacy was observed for the alpha-2 adrenoceptors, although isapirone and a metabolite showed weak affinity, indicating that these compounds might influence the central and peripheral nervous systems through alpha adrenoceptor activity.
$100 - $150
Hourly Rate
Novel anxiolytics discriminate between postsynaptic serotonin receptors mediating different physiological responses on single neurons of the rat hippocampus.
London, UK
2 hours ago
1 Received
- The study investigated how buspirone affects hippocampal pyramidal cells in the CA1 region using in vitro brain slice recordings.
- Buspirone triggered a long-lasting hyperpolarization in the cells that was linked to increased potassium conductance, but it did not replicate all effects of 5-HT, particularly the depolarizing response.
- The findings suggest that buspirone acts as a partial agonist on certain 5-HT receptors and that its effects and those of related compounds can distinguish between different types of serotonergic receptor functions, potentially impacting anxiety treatment.
$100 - $150
Hourly Rate
Identification of the 5-HT1A receptor binding subunit in rat brain membranes using the photoaffinity probe [3H]8-methoxy-2-[N-n-propyl, N-3-(2-nitro-4-azidophenyl)aminopropyl]aminotetralin.
London, UK
2 hours ago
1 Received
- - A new tritiated version of a 5-HT1A photoaffinity probe was created and used to label specific receptor binding sites in rat brain membranes, particularly focusing on the hippocampus.
- - The labeling process incorporated a 63-kilodalton protein, referred to as PI, which showed a strong connection to the 5-HT1A receptor sites, as its labeling could be blocked by specific 5-HT1A ligands but not by other types of drugs.
- - The study concluded that the 63-kilodalton protein PI is likely the binding subunit of the 5-HT1A receptor and contains important sulfhydryl groups that play a critical role in its function.
$100 - $150
Hourly Rate
Benzodiazepines and putative 5-HT1A agonists increase hypertonic saline consumption in rehydrating rats.
London, UK
2 hours ago
1 Received
- Male rats were subjected to a 22-hour water-deprivation schedule before testing their intake of hypertonic NaCl solutions (1.8% or 2.7%).
- The novel benzodiazepine Ro23-0364 significantly increased hypertonic saline consumption without causing sedation, unlike Midazolam, which increased intake but caused sedation at higher doses.
- Three 5-HT1A agonists (8-OH-DPAT, gepirone, and ipsapirone) also elevated salt intake, but higher doses led to a flattened body posture that reduced drinking behavior, suggesting behavioral similarities between these drugs and benzodiazepines in stimulating salt consumption.
$100 - $150
Hourly Rate
Behavioral effects of several new anxiolytics and putative anxiolytics.
London, UK
2 hours ago
1 Received
- The study tested the behavioral effects of new anxiolytic drugs on rats using two different tests sensitive to anxiety relief.
- In the first test, multiple compounds, including diazepam and several others, showed significant effects in increasing rats' lever responses, indicating anxiolytic activity, especially during a stressful situation involving electric shocks.
- In the second test, while diazepam led to similar responses in some drugs, others like buspirone and gepirone did not show the same properties, suggesting that they act differently compared to traditional benzodiazepines.
$100 - $150
Hourly Rate