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Central Nervous System Effects of Essential Oil Compounds
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Elaine Elisabetsky, Domingos S. Nunes
β-pinene 17 diminished immobility in the FST, though it also decreased ambulation in OF (Guzmán-Gutiérrez et al., 2012). The antidepressive-like effect was replicated and extended by the same group, in which the use of antagonists suggests 17 effects are mediated by 5HT1A serotonin receptors (WAY100635), β adrenoceptors (propranolol but not yohimbine), and D1 dopamine receptors (SCH23390) (Guzmán-Gutiérrez et al., 2015).
Preclinical Antidepressant-Like Effects of Terpenes, Polyphenolics, and Other Non-Flavonoid Phytochemicals
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Two weeks of pretreatment with linalool protected rats from the depression-like effects of chronic restraint stress. When subjected to the forced swim test, the treated rats exhibited significantly less immobility.120 Linalool also showed antidepressant-like effects in mice by reducing immobility in the forced swim test. This effect was blocked by the 5-HT1A antagonist, WAY 100635, which suggested a serotonergic contribution.121
Cannabidiol in Mental Health Disorders
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Alline C. de Campos, Felipe V. Gomes, Samia R. Joca, Francisco S. Guimarães
In 2008, we found that the anxiolytic effects of CBD observed after direct injection into the dorsal portions of the periaqueductal gray matter (dPAG) were not mediated by CB1 receptors. Considering that CBD can inhibit the FAAH enzyme (Bisogno et al., 2001), this result came as a surprise for us. We had previously found that AEA, injected into the same site, caused a CB1-mediated anxiolytic response (Moreira et al., 2007). We went on to test if, as had been suggested by Russo et al. (2005), CBD could be acting through 5-HT1A receptors. We found that WAY100635, a 5-HT1A-receptor antagonist, prevented the anxiolytic effects of CBD when injected into this region (Campos and Guimarães, 2008). This antagonist also abolished the panicolytic-like effects of intra-dPAG CBD injections (Soares et al., 2010; Campos et al., 2013a). Since then, 5-HT1A-receptors have been found to mediate CBD acute anti-aversive effects in several other studies using systemic or intra-cerebral (into the prelimbic prefrontal cortex and bed nucleus of the stria terminalis) administration (Fogaça et al., 2014; Gomes et al., 2011, 2012; Zanelati et al., 2010).
Ginsenoside Re attenuates 8-OH-DPAT-induced serotonergic behaviors in mice via interactive modulation between PKCδ gene and Nrf2
Published in Drug and Chemical Toxicology, 2023
Eun-Joo Shin, Ji Hoon Jeong, Bao-Trong Nguyen, Naveen Sharma, Cuong Ngoc Kim Tran, Seung-Yeol Nah, Yi Lee, Jae Kyung Byun, Sung Kwon Ko, Hyoung-Chun Kim
GRe, 8-OH-DPAT (Sigma-Aldrich, St. Louis, MO), and WAY100635 (WAY; Sigma-Aldrich, St. Louis, MO) were dissolved in 0.9% sterile saline immediately prior to use. Rottlerin (Biomol Research Laboratories Inc., Plymouth, PA), a PKCδ inhibitor, was dissolved in dimethyl sulfoxide as a stock solution and then stored at −20 °C, it was diluted in sterile saline immediately before use to 1 μg/μL. Male PKCδ KO and WT mice, weighing approximately 23 ± 2 g, received GRe (10 mg/kg, i.p.) twice a day for five days. Mice received 8-OH-DPAT (2 mg/kg, i.p.) or saline 2 h after the final GRe treatment. The dose of 8-OH-DPAT was determined based on a previous study (Tran et al.2019). Rottlerin (3 μg, i.c.v./brain) was infused 6 and 2 h earlier than 8-OH-DPAT, and WAY (1 mg/kg, i.p.) was injected 30 min before treatment with 8-OH-DPAT. The doses of rottlerin and WAY were determined based on our previous study (Tran et al.2019). In addition, 8-OH-DPAT-induced p-PKCδ expression peaked 1 h after treatment in our previous study (Tran et al.2019). Thus, mice were euthanized by cervical dislocation 1 h after 8-OH-DPAT treatment, and hypothalamic tissues were quickly dissected and frozen immediately in liquid nitrogen. The experimental design is illustrated in Figure 1.
Beneficial effects of atypical antipsychotics on object recognition deficits after adolescent toluene exposure in mice: involvement of 5-HT1A receptors
Published in The American Journal of Drug and Alcohol Abuse, 2022
Mei-Yi Lee, Chung-Pin Hsieh, Ming-Huan Chan, Hwei-Hsien Chen
To test whether activation of 5-HT1A receptors is involved in the beneficial effects of aripiprazole, clozapine, and buspirone to restore the toluene-induced recognition memory deficits, 3 separate experiments were performed. WAY-100635, a 5-HT1A receptor antagonist, was administered 30 min prior to aripiprazole, clozapine, or buspirone in toluene-exposed mice for subsequent NORT. Each experiment included at least 4 groups (oil+vehicle+vehicle, toluene+vehicle+vehicle, toluene+ vehicle+drug, toluene+WAY-100635+drug). WAY-100635 has been reported to alleviate cognitive impairments induced by a fornix lesion (18) or dizocilpine (19). Therefore, the toluene+WAY-100635+vehicle group was included in the experiment of aripiprazole to determine if WAY-100635 alone could restore the detrimental effect of toluene. The numbers of mice used in each experiment were 34 (aripiprazole), 32 (clozapine), and 26 (buspirone).
A definite measure of occupancy exposures, seeking with non-radiolabeled in vivo 5-HT2A receptor occupancy and in vitro free fractions
Published in Journal of Receptors and Signal Transduction, 2018
Gopinadh Bhyrapuneni, Jagadeesh Babu Thentu, Veera Raghava Choudary Palacharla, Nageswararao Muddana, Raghupathi Reddy Aleti, Devender Reddy Ajjala, Ramakrishna Nirogi
Serotonin (5-HT) 2 A receptor subtype occupancy elucidates the current objective. The 5-HT2A receptor occupancy was determined using non-radiolabeled tracer MDL-100,907, a reported PET ligand of 5-HT2A receptors [7,8]. In previous work [9], non-radiolabeled MDL-100,907 was optimized for a treatment dose (3 µg/kg), sacrification time (15 min), and specific/nonspecific brain regions in rats. The 5-HT2A occupancy with either labeled or non-radiolabeled form of MDL-100,907 tracer was comparable. MDL-100,907 was used either as alone or in combination with other target tracers (D2, raclopride, and 5-HT1A, WAY-100635). At those conditions, the tracer binding and 5-HT2A occupancy values are similar [9]. Further, 5-HT2A receptors are involved in the treatment of depression and psychosis. The combination of 5-HT2A receptor blockade with selective serotonin reuptake (SSRI) transporter inhibition reduced the onset of the antidepressant effect of SSRI’s [10]. In the treatment of psychosis with atypical drugs, blockade of 5-HT2A receptors in the nigrostriatal pathway promotes dopaminergic actions and reduce the extrapyramidal effect [11,12].