Gepirone-the latest antidepressant on market state-of-the-art or run-of-the-mill?
Asian J Psychiatr. 2024 Feb 3;94:103937. doi: 10.1016/j.ajp.2024.103937. Online ahead of print.ABSTRACTGepirone was recently launched and FDA-approved for MDD. It belongs to azapirones group of psychotropics that is in popular use in Japan and China. Here, author wraps up current knowledge on gepirone contrasted with the older and cheaper anxiolytic buspirone.PMID:38335641 | DOI:10.1016/j.ajp.2024.103937 (Source: Asian Journal of Psychiatry)
Source: Asian Journal of Psychiatry - February 9, 2024 Category: Psychiatry Authors: Ahmed Naguy Source Type: research

Inhibitory Actions of Antidepressants, Hypnotics, and Anxiolytics on Recombinant Human Acetylcholinesterase Activity
Biol Pharm Bull. 2024;47(1):328-333. doi: 10.1248/bpb.b23-00719.ABSTRACTAlzheimer's disease (AD) is accompanied by behavioral and psychological symptoms of dementia (BPSD), which is often alleviated by treatment with psychotropic drugs, such as antidepressants, hypnotics, and anxiolytics. If these drugs also inhibit acetylcholinesterase (AChE) activity, they may contribute to the suppression of AD progression by increasing brain acetylcholine concentrations. We tested the potential inhibitory effects of 31 antidepressants, 21 hypnotics, and 12 anxiolytics on recombinant human AChE (rhAChE) activity. At a concentration of 1...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Keisuke Obara Haruka Mori Suzune Ihara Kento Yoshioka Yoshio Tanaka Source Type: research

Buspirone for the treatment of anxiety in Williams syndrome: a retrospective chart review study
CONCLUSIONS: In this retrospective study, the majority of patients responded to a 16-week course of buspirone. Prospective studies are warranted to further assess the efficacy and tolerability of buspirone for anxiety in WS.PMID:38247447 | DOI:10.1080/14656566.2024.2308678 (Source: Expert Opinion on Pharmacotherapy)
Source: Expert Opinion on Pharmacotherapy - January 22, 2024 Category: Drugs & Pharmacology Authors: Eva Shin Danielle Renzi Camila Canales Caitlin Ravichandran Christopher J McDougle Robyn P Thom Source Type: research

Preparation, Swelling, and Drug Release Studies of Chitosan-based Hydrogels for Controlled Delivery of Buspirone Hydrochloride
CONCLUSION: The results showed that the developed chitosan-based hydrogel can be considered one of the most suitable drug carrier systems for the controlled delivery of buspirone.PMID:38204236 | DOI:10.2174/0113892010267638231206164415 (Source: Current Pharmaceutical Biotechnology)
Source: Current Pharmaceutical Biotechnology - January 11, 2024 Category: Biotechnology Authors: Muhammad Suhail Chih-Wun Fang I-Hui Chiu Hamid Ullah I-Ling Lin Ming-Jun Tsai Pao-Chu Wu Source Type: research

FDA Approves Exxua for Treatment of Major Depression in Adults
The Food and Drug Administration (FDA) late last monthapproved a medication called Exxua (gepirone) for the treatment of major depression in adults. (Gepirone is in the same class of medications as the anti-anxiety medication buspirone.)The medication, available in extended-release tablets, is “the first and only approved antidepressant with a novel mechanism of action that selectively targets the serotonin 1A receptor, a key regulator of mood and emotion,” according to apress release by the Fabre-Kramer Pharmaceuticals, maker of Exxua.The FDA approval was based, in part, on two eight-week randomized, double-blind, pla...
Source: Psychiatr News - October 2, 2023 Category: Psychiatry Tags: adults antidepressant Exxua FDA Food and Drug Administration major depression serotonin 1A side effects Source Type: research

Functional consequences of a rare human serotonergic 5-HT1A receptor variant
Serotonin (5-HT) plays a central role in various brain functions via the activation of a family of receptors, most of them G protein coupled receptors (GPCRs). 5-HT1A receptor, the most abundant 5-HT receptors, was implicated in many brain dysfunctions and is a major target for drug discovery. Several genetic polymorphisms within the 5-HT1A receptor gene were identified and linked to different conditions, including anxiety and depression. Here, we used Xenopus oocytes to examine the effects of one of the functional polymorphism, Arg220Leu, on the function of the receptor. We found that the mutated receptor shows normal act...
Source: Frontiers in Pharmacology - September 18, 2023 Category: Drugs & Pharmacology Source Type: research

Incorporation and performance verification of hepatic portal blood flow shunting in minimal and full PBPK models of liver cirrhosis
The objectives of this work were to implement a Physiologically Based Pharmacokinetic (PBPK) framework describing shunted blood flows in virtual patients with differing degrees of liver cirrhosis; and to assess the minimal and full PBPK models performance using drugs with intermediate to high hepatic extraction. Single dose concentration-time profiles and PK parameters for oral Ibrutinib, midazolam, propranolol and buspirone were simulated in Healthy-Volunteer (HV) and subjects with cirrhosis (Child-Pugh severity score A, B or C). Model performance was verified by comparing predicted to observed fold-changes in PK paramete...
Source: Clinical Pharmacology and Therapeutics - August 24, 2023 Category: Drugs & Pharmacology Authors: Ben G Small Oliver Hatley Masoud Jamei Iain Gardner Trevor N Johnson Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research

Time-Dependent Effects of Buspirone versus Desipramine on the 5-Choice Serial Reaction Time Task in Rats Reared in Social Isolation: Implication of Early Life Experience and Motoric Impulsivity
CONCLUSIONS: Buspirone but not desipramine-induced time-dependent effects of motoric waiting impulsivity can be reversed by IR, indicating a role for early life social experience on 5-HT1A receptor-associated ability to control impulsiveness.PMID:37519173 | DOI:10.31083/j.jin2204080 (Source: Journal of Integrative Neuroscience)
Source: Journal of Integrative Neuroscience - July 31, 2023 Category: Neuroscience Authors: Che-Se Tung You-Wei Lin Chen-Cheng Lin Yia-Ping Liu Source Type: research