Stimulant posterior

Hi-receptors in the adrenal medulla stimulates the release of the two catecholamines noradrenaline and adrenaline as well as enkephalins. In the heart, histamine produces negative inotropic effects via Hr receptor stimulation, but these are normally masked by the positive effects of H2-receptor stimulation on heart rate and force of contraction. Histamine Hi-receptors are widely distributed in human brain and highest densities are found in neocortex, hippocampus, nucleus accumbens, thalamus and posterior hypothalamus where they predominantly excite neuronal activity. Histamine Hrreceptor stimulation can also activate peripheral sensory nerve endings leading to itching and a surrounding vasodilatation ( flare ) due to an axonal reflex and the consequent release of peptide neurotransmitters from collateral nerve endings. 

The posterior pituitary is innervated by direct nervous stimulation from the hypothalamus, resulting in the release of specific hormones. The hypothalamus synthesizes two hormones, oxytocin and vasopressin. These hormones are stored in and released from the posterior pituitary lobe. Oxytocin exerts two actions (1) it promotes uterine contractions during labor, and (2) it contracts the smooth muscles in the breast to stimulate the release of milk from the mammary gland during lactation. Vasopressin is an antidiuretic hormone (ADH) essential for proper fluid and electrolyte balance in the body. Specifically, vasopressin increases the permeability of the distal convoluted tubules and collecting ducts of the nephrons to water. This causes the kidney to excrete less water in the urine. Consequently, the urine becomes more concentrated as water is conserved. 

Vasopressin is a peptide hormone produced by the hypothalamus and secreted by the posterior pituitary in response to stimulation. Normal stimuli for vasopressin release are hyperosmolarity and hypovolemia, with thresholds for secretion of greater than 280 mOsm/kg and greater than 20% plasma volume depletion. A number of other stimuli, such as pain, nausea, epinephrine, and numerous drugs, induce release of vasopressin. Vasopressin release is inhibited by volume expansion, ethanol, and norepinephrine. The physiological effect of vasopressin is to promote free water clearence by altering the permeability of the renal collecting duct to water. In addition, it has a direct vasoconstrictor effect. Consequently, vasopressin results in water retention and volume restoration. In patients with septic shock, vasopressin is appropriately secreted in response to hypovolemia and to elevated serum osmolarity (R14). 

Histamine-containing neurons, located in the tuberomammillary nuclei (TMN) of the posterior hypothalamus, stimulate cortical activation through... 

As noted above, MDA is a potent stimulator of monoamine release (see Table 7.1), and recent reports indicate that a number of MDMA metabolites are bioactive. For example, Forsling et al.61 showed that the metabolite 4-hydroxy-3-methoxymethamphetamine (HMMA) is more potent than MDMA as a stimulator of vasopressin secretion from rat posterior pituitaries in vitro. The neuroendocrine effects produced by in vivo administration of MDMA metabolites have not been examined. Monks et al.62 demonstrated that catechol metabolites of MDMA and MDA, namely, 3,4-dihydroxymethamphetamine (HHMA) and 3,4-dihydroxyamphetamine (HHA), exhibit neurotoxic properties when oxidized and conjugated with glutathione. Further characterization of the biological effects of MDMA metabolites is an important area of research. 

In moths, it was discovered in Helicoverpa zea that a peptide produced in the subesophageal ganglion portion of the brain complex regulates pheromone production in female moths (19). This factor has been purified and characterized in three species, Helicoverpa zea (20), Bombyx mori (21, 22), and Lymantria dispar (23). They are all a 33- or 34-amino acid peptide (named pheromone biosynthesis activating neuropeptide, PBAN) and have in common an amidated C-terminal 5-amino acid sequence (FXPRL-amide), which is the minimum peptide fragment required for pheromon-tropic activity. In the redbanded leafroller moth, it was shown that PBAN from the brain stimulates the release of a different peptide from the bursae copulatrix that is used to stimulate pheromone production in the pheromone gland found at the posterior tip of the abdomen (24). 

Neuropeptides are often grouped by their structural similarity or tissue source. Among these are the hypothalamic releasing factors (e.g., corticotrophin-releasing factor [CRF], thyrotropin-releasing hormone), anteior pituitary hormones (e.g., adrenocorticotrophic hormone [ACTFI], follicle-stimulating hormone [FSFI]), and posterior pituitary hormones... 

Plasma prolactin levels are reduced with acute treatment and remain suppressed after 28 days of chronic treatment (Murphy et al. 1998). With acute treatment, no effects are seen on plasma luteinizing hormone or testosterone levels. However, chronic dietary 5% ginseng increases testosterone levels in male rats (Fahim et al. 1982). Chronic ginsenosides do not alter posterior pituitary hormones oxytocin and vasopressin (Zierer 1991). Similarly, human males administered ginseng extract showed an increase in plasma testosterone, dihydrotestosterone, follicle-stimulating hormone, and luteinizing hormone, but a decrease in prolactin (Salvati et al. 1996). 

Posterior pituitary Two hormones, vasopressin and oxytocin, are synthesised in the hypothalamus and then transported through nerve axons to the posterior pituitary, where they are stored until released. Vasopressin acts on the kidney to conserve water. Its secretion is stimulated by thirst and a decrease in blood pressure. Secretion of oxytocin initiates uterine contraction for parturition. It also stimulates milk ejection from the mammary glands. 

ADH, a nonapeptide, released from the posterior pituitary gland promotes re-absorption of water in the kidney. This response is mediated by vasopressin receptors of the V2 subtype. ADH enhances the permeability of collecting duct epithelium for water (but not for electrolytes). As a result, water is drawn from urine into the hyperosmolar inter-stitium of the medulla. Nicotine augments (p. 110) and ethanol decreases ADH release. At concentrations above those required for antidiuresis, ADH stimulates smooth musculature, including that of blood vessels ( vasopressin ). The latter response is mediated by receptors of the Vi subtype. Blood pressure rises coronary vasoconstriction can precipitate angina pectoris. Lypres-sin (8-L-lysine vasopressin) acts like ADH. Other derivatives may display only one of the two actions. 

Oxytocin (Pitocin, Syntocinon) is a cyclic 8-amino acid peptide that is synthesized in the paraventricular nucleus of the hypothalamus and transported within hypothalamic neurons (in association with neurophysin) to the posterior pituitary for storage. Its mechanism of action involves the direct stimulation of oxytocin receptors found on the myometrial cells. Oxytocin circulates unbound in the plasma, where it has a half-Ufe of approximately 15 minutes. It is primarily inactivated in the kidneys and liver. 

Because dinoprostone produces cervical ripening along with stimulation of the uterus, it has been used as an alternative to oxytocin for the induction of labor. Preparations of dinoprostone can be placed in either the cervix or the posterior fornix. Prepidil is a formulation and delivery system of dinoprostone that delivers a dose of 0.5 mg into the cervix, while Cervidil consists of the drug embedded in a plastic matrix. The matrix is designed to deliver a dose of 0.3 mg per hour for 12 hours. 

Mechanism of Action A posterior pituitary hormone that increases reabsorption of water by the renal tubules. Increases water permeability at the distal tubule and collecting duct. Directly stimulates smooth muscle in the GI tract. Therapeutic Effect Causes peristalsis and vasoconstriction. 

Drugs such as amphetamine and methylphenidate act to enhance the release and/or inhibit the reuptake of both DA and NE. An extensive review of stimulant actions and their relevance to ADHD can be found in Solanto et al. (2001). Methylphenidate can improve PFC working memory function in healthy adult humans and animals (Mehta et ah, 2000). It is likely that these improvements are due to both DA and NE beneficial actions in PFC, as well as stimulation of posterior association cortices. Some of the ideas regarding the sites of stimulant therapeutic actions in the brain are illustrated in Figure 8.2. 

However, the posterior cortical areas may be aided by P and aj-adrenergic receptor stimulation and by dopaminergic stimulation, and thus stimulants may promote the attentional processing abilities of these areas. It is important to note that there has been no direct animal research on catecholamine modulation of posterior cortical function thus this idea remains speculative. 

Oxytocin, a nine amino acid peptide, is synthesized primarily in the paraventricular and supraoptic (SON) nuclei of the hypothalamus, from which it is released to the general circulation through the posterior pituitary (Insel et ah, 1997). However, oxytocinergic fibers have also been found to project from the PVN to the limbic system and several autonomic centers in the brain stem. This central OT pool appears to be independent of pituitary OT release cerebrospinal fluid (CSF) and plasma OT responses to numerous stimuli are not correlated (Insel, 1997). Oxytocin and its analog (or partner) peptide vasopressin are found only in mammals. A related peptide, vasotocin, thought to be the evolutionary precedent of these peptides, is found in reptiles and birds. The first known actions of OT were its peripheral effects on the physiology of new mothers. In mammals, OT stimulates milk ejection and uterine contraction, essential aspects of maternal physiology (Insel et ah, 1997). 

The anterior lobe secretes various trophic hormones, the posterior lobe is responsible for the secretion of oxytocin and antidiuretic hormone (vasopressin) and middle lobe secretes melanocyte-stimulating hormone (MSH) which may affect the synthesis of melanin. 

Oxytocin is a peptide hormone secreted by the posterior pituitary that participates in labor and delivery and elicits milk ejection in lactating women. During the second half of pregnancy, uterine smooth muscle shows an increase in the expression of oxytocin receptors and becomes increasingly sensitive to the stimulant action of endogenous oxytocin. Pharmacologic concentrations of oxytocin powerfully stimulate uterine contraction. 

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