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Interaction of Drugs of Dependence With Receptors
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
We suggest that the receptor-associated effects produced by LSD occur in the following sequence: a. Postsynaptic binding to the physiological 5-HT receptor.b. Blockade of the release of 5-HT, possibly mediated at the level of the 5-HT storage site (vesicle).c. Release and depletion of NE stores.d. Stimulation of dopaminergic pathways due to disinhibition resulting from depression of adrenergic outflow.
Psychopharmacology EMIs
Published in Michael Reilly, Bangaru Raju, Extended Matching Items for the MRCPsych Part 1, 2018
Each option may be used once, more than once or not at all.Select the agent above that matches each of the following pharmacodynamic profiles.Entry of cells via sodium channels and inhibition of the phosphoinositide second messenger system.Interference with sodium and calcium channels thereby enhancing the function of GABA and reducing that of glutamate. Also, inhibition of carbonic anhydrase.Inhibition of cAMP production and potentiation of serotonin (5-HT) responses by increasing 5-HT release and increasing 5-HT receptor sensitivity.
Questions and Answers
Published in David Browne, Brenda Wright, Guy Molyneux, Mohamed Ahmed, Ijaz Hussain, Bangaru Raju, Michael Reilly, MRCPsych Paper I One-Best-Item MCQs, 2017
David Browne, Brenda Wright, Guy Molyneux, Mohamed Ahmed, Ijaz Hussain, Bangaru Raju, Michael Reilly
Answer: C. Anticipation does occur in depression. Twin, family and adoption studies support the genetic theory of depression but environmental factors are very important too. Kendler found that genetic factors increase the risk of onset of depression by increasing the sensitivity of individuals to the depression-inducing effects of life events. 5-HT receptor polymorphisms and allelic association between the serotonin transporter gene and unipolar depression have been found. [M. p. 704; T. p. 302]
Long-term safety and efficacy, including anhedonia, of vortioxetine for major depressive disorder: findings from two open-label studies
Published in Current Medical Research and Opinion, 2023
Gregory W. Mattingly, Oscar Necking, Simon Nitschky Schmidt, Elin Reines, Hongye Ren
Vortioxetine is a multimodal antidepressant with a pharmacological profile that is distinct from other currently available antidepressants. It acts as an inhibitor of the serotonin (5-HT) transporter as well as modulating the activity of multiple 5-HT receptor subtypes, and also mediates its therapeutic effects via the norepinephrine, dopamine, amino acids, histamine, and cholinergic systems3–5. Currently approved at doses between 5 mg and 20 mg, the efficacy, safety and tolerability of vortioxetine versus placebo in managing depressive symptoms has been established in a large clinical development program including more than 12,000 patients with MDD6–19. In the long-term, maintenance treatment with vortioxetine has been shown to maintain and further improve the efficacy established during acute treatment with vortioxetine. In a pooled analysis of five studies, the total response rate was 75% and the total remission rate was 61% at one year20. Importantly, efficacy was consistent across patient subgroups regardless of gender, age, initial level of depressive or anxiety symptoms, number of previous major depressive episodes (MDEs), or duration of the current MDE. Long-term maintenance treatment with vortioxetine has also been proven effective in preventing relapse of MDD and is well tolerated21.
Analgesic and anti-inflammatory effects of modafinil in a mouse model of neuropathic pain: A role for nitrergic and serotonergic pathways
Published in Neurological Research, 2022
Hossein Ghorbanzadeh, Parastoo Mohebkhodaei, Mehran Nematizadeh, Nastaran Rahimi, Mahsa Rafeiean, Mehdi Ghasemi, Ahmad R. Dehpour
Several lines of evidence have indicated serotonin involvement in pain processing pathways over the past years. It was reported that topical administration of ondansetron, a 5-HT3 receptor antagonist, exerts anti-inflammatory and antinociceptive effects in a model of inflammatory pain following intradermal injection of capsaicin in humans [48]. Other investigations also showed that granisetron, another 5-HT3 receptor antagonist, abolished serotonin-induced hyperalgesia and allodynia in human masseter muscle [49]. While serotonin’s peripheral hyperalgesic effect is somehow confirmed, its effect on central pain transmission and perception depends on the pain condition [50]. In our study, modafinil’s alleviative effect on neuropathic pain was reversed after pretreatment with citalopram. Besides, citalopram blocked the modafinil suppressive effects on TNF-α concentration in the cuffed sciatic nerve. These data may suggest that modafinil modulates serotonergic activities concurrent with its anti-inflammatory effects. Clearly, more detail studies using specific 5-HT receptor subtype agonists and antagonists (e.g. 5-HT3 receptor modulators) are needed to more deeply explore these findings.
Sumatriptan improves the locomotor activity and neuropathic pain by modulating neuroinflammation in rat model of spinal cord injury
Published in Neurological Research, 2021
Khashayar Afshari, Amir Dehdashtian, Nazgol-Sadat Haddad, Seyedeh Zarifeh Jazaeri, Daniel C. Ursu, Mina Khalilzadeh, Arvin Haj-Mirzaian, Saeed Shakiba, Terry C Burns, Seyed Mohammad Tavangar, Mehdi Ghasemi, Ahmad Reza Dehpour
NP is known as a common secondary complication of SCI [5]. One of the important neurotransmitters that has been shown to be involved in NP is serotonin (5-hydroxytryptamine, 5-HT) [5,6]. Brain stem-originated 5-HT is shown to hamper sensory afferent transmissions and their related spinal reflexes [7]; accordingly, pathologic conditions such as SCI disinhibit sensory transmission and cause NP through eradicating this 5-HT innervation [5,6]. Additional evidence also suggests that 5-HT release and 5-HT receptors activation within the spinal cord anterior horn contribute to the motor function and locomotor control [7]. Moreover, 5-HT functions as an immunomodulatory agent which exerts this effect through inhibiting oxidative stress and inflammatory cytokines generation and release as well as modulating immune cells migration [8–10]. Different 5-HT receptor subtypes have been identified to mediate the immunomodulatory effects of 5-HT. For instance, activation of 5-HT3, 5-HT4 and 5-HT7 receptor subtypes on human monocytes regulates inflammation and production of cytokines such as TNF-α and IL-1β [10,11]. An in vivo study on systemic TNF-α− treated rats found that 5-HT2A receptor activation blocked the expression of pro-inflammatory markers, e.g. IL-6 and IL-1b, in both aortic arch and small intestine as well as blood IL-6 levels in these animals [11].