5-HT Receptors and Temperature Homeostasis

Voronova, Irina P.

doi:10.3390/biom11121914

Cited by 18 publications

(11 citation statements)

References 241 publications

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“…Some authors understand SS as a consequence of excessive activation of 5-HT2A receptors [ 49 ]. The available evidence supports the view that activation of these receptors is associated with hyperthermia, while inhibition of the same favors hypothermia [ 10 , 50 , 51 ].…”

Section: Neurotransmitterssupporting

confidence: 68%

“…Voronova, 2021 states that 5-HT1A activation, as a rule, leads to the development of hypothermia in animals at warm ambient temperature [ 10 ]. Antagonism at these receptors by cyproheptadine (Ki ≈ 60 nm) in the context of SS does not appear to be beneficial or desirable ( Figure 3 ).…”

Section: Neurotransmittersmentioning

confidence: 99%

“…Activation of central 5-HT3 receptors are effective in hypothermia induction due to marked decrease in thermogenesis and increase in heat loss. The implication of central 5-HT3 receptors in thermoregulation and the interaction with 5-HT1A receptors was reported [ 10 , 54 ]; a centrally administered 5-HT3 agonist dose-dependently reduced temperature [ 55 ]. Voronova, 2021 concludes that, “all available data indicate that central 5-HT3 receptors activation leads to a decrease in body temperature of a warm-blooded organism, and this occurs due to a decrease in heat production and an increase in heat loss.” [ 10 ] ( Figure 5 ).…”

Section: Neurotransmittersmentioning

confidence: 99%

“…Must read reviews on the topic, such as the ones authored by Trevor and Barnes and by Voronova, exist [ 10 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

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Hyperthermia and Serotonin: The Quest for a “Better Cyproheptadine”

Petroianu

2022

IJMS

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Fine temperature control is essential in homeothermic animals. Both hyper- and hypothermia can have deleterious effects. Multiple, efficient and partly redundant mechanisms of adjusting the body temperature to the value set by the internal thermostat exist. The neural circuitry of temperature control and the neurotransmitters involved are reviewed. The GABAergic inhibitory output from the brain thermostat in the preoptic area POA to subaltern neural circuitry of temperature control (Nucleus Raphe Dorsalis and Nucleus Raphe Pallidus) is a function of the balance between the (opposite) effects mediated by the transient receptor potential receptor TRPM2 and EP3 prostaglandin receptors. Activation of TRPM2-expressing neurons in POA favors hypothermia, while inhibition has the opposite effect. Conversely, EP3 receptors induce elevation in body temperature. Activation of EP3-expressing neurons in POA results in hyperthermia, while inhibition has the opposite effect. Agonists at TRPM2 and/or antagonists at EP3 could be beneficial in hyperthermia control. Activity of the neural circuitry of temperature control is modulated by a variety of 5-HT receptors. Based on the theoretical model presented the “ideal” antidote against serotonin syndrome hyperthermia appears to be an antagonist at the 5-HT receptor subtypes 2, 4 and 6 and an agonist at the receptor subtypes 1, 3 and 7. Very broadly speaking, such a profile translates in a sympatholytic effect. While a compound with such an ideal profile is presently not available, better matches than the conventional antidote cyproheptadine (used off-label in severe serotonin syndrome cases) appear to be possible and need to be identified.

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Section: Neurotransmitterssupporting

confidence: 68%

Section: Neurotransmittersmentioning

confidence: 99%

Section: Neurotransmittersmentioning

confidence: 99%

“…Must read reviews on the topic, such as the ones authored by Trevor and Barnes and by Voronova, exist [ 10 , 11 ].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Hyperthermia and Serotonin: The Quest for a “Better Cyproheptadine”

Petroianu

2022

IJMS

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“…Ionotropic 5-HT receptors are selectively permeable to K + , Na + and Ca 2+ after interacting with ligands, which can activate neurons [ 85 ]. 5-HT receptors are widely distributed in the cortex, thalamus and hippocampus, and ionotropic 5-HT receptors are also distributed in the periphery [ 86 ].…”

Section: Neurotransmitter Abnormalities and Cognitive Dysfunctionmentioning

confidence: 99%

Neurotransmitters in Prevention and Treatment of Alzheimer’s Disease

Yang

Zou

Wang

2023

IJMS

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Alzheimer’s disease (AD) is the most frequent cause of cognitive impairment in middle-aged and older populations. There is a lack of drugs that demonstrate significant efficacy in AD, so the study of the pathogenesis of AD is of great importance. More efficacious interventions are needed, as reflected by our population’s fast aging. Synaptic plasticity is the capacity of neurons to adjust their connections, and it is strongly tied to learning and memory, cognitive function, and brain injury recovery. Changes in synaptic strength, such as long-term potentiation (LTP) or inhibition (LTD), are thought to represent the biological foundation of the early stages of learning and memory. The results of numerous studies confirm that neurotransmitters and their receptors play an important role in the regulation of synaptic plasticity. However, so far, there is no definite correlation between the function of neurotransmitters in aberrant neural oscillation and AD-related cognitive impairment. We summarized the AD process to understand the impact of neurotransmitters in the progression and pathogenesis of AD, including the current status of neurotransmitter target drugs, and the latest evidence of neurotransmitters’ function and changes in the AD process.

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Pharmaco-toxicological effects of the novel tryptamine hallucinogen 5-MeO-MiPT on motor, sensorimotor, physiological, and cardiorespiratory parameters in mice—from a human poisoning case to the preclinical evidence

Bassi,

Bilel,

Tirri

et al. 2024

Psychopharmacology

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Rationale The 5-methoxy-N-methyl-N-isopropyltryptamine (5-MeO-MiPT, known online as “Moxy”) is a new psychedelic tryptamine first identified on Italian national territory in 2014. Its hallucinogen effects are broadly well-known; however, only few information is available regarding its pharmaco-toxicological effects. Objectives Following the seizure of this new psychoactive substances by the Arm of Carabinieri and the occurrence of a human intoxication case, in the current study we had the aim to characterize the in vivo acute effects of systemic administration of 5-MeO-MiPT (0.01–30 mg/kg i.p.) on sensorimotor (visual, acoustic, and overall tactile) responses, thermoregulation, and stimulated motor activity (drag and accelerod test) in CD-1 male mice. We also evaluated variation on sensory gating (PPI, prepulse inhibition; 0.01–10 mg/kg i.p.) and on cardiorespiratory parameters (MouseOx and BP-2000; 30 mg/kg i.p.). Lastly, we investigated the in silico ADMET (absorption, distribution, metabolism, excretion, toxicity) profile of 5-MeO-MiPT compared to 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DIPT) and N,N-dimethyltryptamine (DMT). Results This study demonstrates that 5-MeO-MiPT dose-dependently inhibits sensorimotor and PPI responses and, at high doses, induces impairment of the stimulated motor activity and cardiorespiratory changes in mice. In silico prediction shows that the 5-MeO-MiPT toxicokinetic profile shares similarities with 5-MeO-DIPT and DMT and highlights a cytochrome risk associated with this compound. Conclusions Consumption of 5-MeO-MiPT can affect the ability to perform activities and pose a risk to human health status, as the correspondence between the effects induced in mice and the symptoms occurred in the intoxication case suggests. However, our findings suggest that 5-MeO-MiPT should not be excluded from research in the psychiatric therapy field.

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5-HT Receptors and Temperature Homeostasis

Cited by 18 publications

References 241 publications

Hyperthermia and Serotonin: The Quest for a “Better Cyproheptadine”

Hyperthermia and Serotonin: The Quest for a “Better Cyproheptadine”

Neurotransmitters in Prevention and Treatment of Alzheimer’s Disease

Pharmaco-toxicological effects of the novel tryptamine hallucinogen 5-MeO-MiPT on motor, sensorimotor, physiological, and cardiorespiratory parameters in mice—from a human poisoning case to the preclinical evidence

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