How to unblock serotonin receptors?

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Journal Article•DOI Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs B. P. Richardson, G. Engel, P. Donatsch, P. A. Stadler - Show less +3 more 11 Jul 1985-Nature 845 Citations	We describe a new class of drugs that selectively block serotonin M-receptors on peripheral neurones.
Journal Article•DOI Rodent data and general hypothesis: antipsychotic action exerted through 5-Ht2A receptor antagonism is dependent on increased serotonergic tone. Peter Martin, Nicholas Waters, C. J. Schmidt, Arvid Carlsson, Maria L. Carlsson - Show less +4 more 01 Jan 1998-Journal of Neural Transmission 85 Citations	M100907, by blocking 5-HT2A receptors, unveils the inhibitory effect exerted on locomotion by these other serotonin receptors.
Journal Article•DOI Evaluation of serotonin-2A receptor occupancy with 123I-5-I-R91150 and single-photon emission tomography before and after low-dose pipamperone administration in the canine brain. Kathelijne Peremans, Bart De Spiegeleer, Erik Buntinx, André Dobbeleir, Simon Vermeire, Eva Vandermeulen, Filip De Vos, Anton Megens, Jos Eersels, Kurt Audenaert - Show less +9 more 01 Aug 2008-Nuclear Medicine Communications 11 Citations	This experiment supports the hypothesis that pipamperone, even in the low-dose range, significantly blocks serotonin-2A receptors.
Journal Article•DOI Antidepressants for the treatment of insomnia : a suitable approach? Michael H. Wiegand 01 Jan 2008-Drugs 97 Citations	Drugs blocking serotonin 5-HT2A or 5-HT2C receptors should be preferred over those whose sedative property is caused by histamine receptor blockade only.
Journal Article•DOI Medication treatment in subjects with autistic spectrum disorders. Jan K. Buitelaar, Sophie H. N. Willemsen-Swinkels - Show less +1 more 01 Jan 2000-European Child & Adolescent Psychiatry 73 Citations	Pharmacological interventions with serotonin reuptake blockers or with atypical neuroleptics that block both dopamine (D2) and serotonin (5-HT2) receptors seem to offer clinical benefit and merit further study.
Journal Article•DOI Opposite regulation of serotonin-S2 and dopamine-D2 receptors in rat brain following chronic receptor blockade. J. E. Leysen, P. Van Gompel, D. Chaffoy de Courcelles, Carlos J. E. Niemegeers - Show less +3 more 01 Jan 1987 23 Citations	These observations demonstrate that in contrast to the receptor regulation theory, serotonin-S2 receptors are down regulated following persistent receptor blockade.
Journal Article•DOI Serotonin-dependent maintenance of spatial performance and electroencephalography activation after cholinergic blockade: effects of serotonergic receptor antagonists. Hans C. Dringenberg, Robert M. Zalan - Show less +1 more 07 Aug 1999-Brain Research 32 Citations	The results suggest that a concurrent blockade of multiple 5-HT receptors, but not selective blockade of serotonin(1A) or serotonin(2) receptors alone, mimics the ability of global 5-HT depletion to abolish behavioral capacities that are resistant to muscarinic receptor blockade.
Book Chapter•DOI Influence of Serotonin on the Blood–Brain and the Blood–Spinal Cord Barriers Hari Shanker Sharma 01 Jan 2004 18 Citations	This effect of serotonin is mediated via serotonergic receptors.
Journal Article•DOI Hot flushes and serotonin Hemmie H.G. Berendsen 01 Mar 2002-British Menopause Society Journal 43 Citations	The neurotransmitter serotonin seems to be especially involved.
Journal Article•DOI Blocking effects of cyproheptadine and methysergide upon two different cardiovascular responses to serotonin. Gilbert R. Hageman, Thomas N. James, Ferdinand Urthaler - Show less +2 more 01 Dec 1980-Experimental Biology and Medicine 8 Citations	The differential blocking effectiveness of these two serotonin antagonists suggests an important difference in physiological characteristics of the serotonin receptors involved.

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There is no consistent evidence linking lowered serotonin concentrations or activity to depression, as suggested by various studies. The serotonin hypothesis of depression, which posits a direct association between serotonin levels and depressive symptoms, has been extensively scrutinized. Research indicates that depression may not be caused by decreased serotonin activity, with some studies even suggesting that long-term antidepressant use could reduce serotonin concentration. Additionally, investigations into the effects of specific genetic variations related to the serotonergic and endocannabinoid systems have shown potential susceptibility to depression in carriers of certain alleles. Overall, the current body of evidence does not strongly support the notion that lowered serotonin concentrations or activity are directly linked to the development of depression.How CBD is absorbed in the gut?

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Cannabidiol (CBD) absorption in the gut is influenced by several factors, including the presence of food, the formulation of CBD, and the activity of the endocannabinoid system. Studies have shown that the bioaccessibility of CBD significantly increases when consumed with food, particularly high-fat meals, which enhance its micellarization efficiency and, consequently, its absorption through the gut wall. This is attributed to the lipase enzyme activity and the presence of bile salts, which facilitate the formation of micelles from hydrolyzed lipids, aiding in the bioaccessibility of hydrophobic molecules like CBD. Furthermore, the development of novel nanoemulsion preparations of CBD has been shown to improve its poor solubility and absorption, demonstrating a significant increase in the area under the curve (AUC) and maximum concentration (Cmax) in pharmacokinetic profiles compared to conventional CBD oil formulations. This suggests that nanoemulsion formulations can enhance CBD absorption regardless of bile secretion, which is essential for the micelle formation required for the absorption of conventional CBD oil. The endocannabinoid system also plays a crucial role in the absorption and bioavailability of CBD. Activation of cannabinoid receptors in the gut can influence gastrointestinal motility and secretion, potentially affecting the absorption of CBD. Moreover, the modulation of this system can impact the permeability of the intestinal epithelium, which is critical for the absorption of substances from the gut. In summary, CBD absorption in the gut is enhanced by the presence of food, particularly fats that stimulate bile and lipase activity, improving CBD's solubility and bioaccessibility. Nanoemulsion formulations further enhance CBD absorption by overcoming its poor solubility. Additionally, the endocannabinoid system's modulation of gut permeability and motility may also influence CBD absorption.What is the correlation between cortisol levels and cholesterol levels in humans?

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The correlation between cortisol levels and cholesterol levels in humans has been extensively studied. Research indicates that there is a significant relationship between cortisol and cholesterol in individuals with metabolic syndrome (MS). Additionally, findings suggest a positive association between serum cholesterol levels and cortisol responses, especially in males, which may impact serotonergic receptor function. Moreover, hormonal mechanisms involving cortisol and cholesterol metabolism appear to be operative in individuals with coronary artery disease (CAD) and Type A-1 behavior pattern, indicating a significant association between cortisol and cholesterol in these populations. Furthermore, cortisol excretion rate correlates with cholesterol levels, blood pressure, and cardiovascular risk factors, highlighting the role of glucocorticoids in regulating key components of cardiovascular health in normal individuals.

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