Feeding receptor

By contrast, neither PP nor NPY-OH, an analogue in which the C-terminal tyrosine-amide has been substituted by tyrosine, were recognized by these two receptor types. The feeding receptor recognizes PYY as well, while the Y3 receptor does not bind PYY (Table 1). The PP1 /Y4 receptor binds PYY better than NPY, however, both lack affinity compared to PP (Gehlert and Hipskind, 1995). 

Y1 affinity/antagonism Y2 affinity/antagonism Feeding receptor affinity/antagonism... 

Nonspecific immunosuppressive therapy in an adult patient is usually through cyclosporin (35), started intravenously at the time of transplantation, and given orally once feeding is tolerated. Typically, methylprednisone is started also at the time of transplantation, then reduced to a maintenance dose. A athioprine (31) may also be used in conjunction with the prednisone to achieve adequate immunosuppression. Whereas the objective of immunosuppression is to protect the transplant, general or excessive immunosuppression may lead to undesirable compHcations, eg, opportunistic infections and potential malignancies. These adverse effects could be avoided if selective immunosuppression could be achieved. Suspected rejection episodes are treated with intravenous corticosteroids. Steroid-resistant rejection may be treated with monoclonal antibodies (78,79) such as Muromonab-CD3, specific for the T3-receptor on human T-ceUs. Alternatively, antithymocyte globulin (ATG) may be used against both B- and T-ceUs. 

The class III cytokine receptor family includes two TNE receptors, the low affinity NGE receptor and 7-ceU surface recognition sites that appear to play a role in proliferation, apoptosis, and immunodeficiency. TNE-a (- 17, 000 protein) is produced by astrocytes and microglia and can induce fever, induce slow-wave sleep, reduce feeding, stimulate prostaglandin synthesis, stimulate corticotrophin-releasing factor and prolactin secretion, and reduce thyroid hormone secretion. TNE-a stimulates IL-1 release, is cytotoxic to oligodendrocytes, and reduces myelination this has been impHcated in multiple sclerosis and encephalomyelitis. Astrocyte TNE-a receptors mediate effects on IL-6 expression and augment astrocytic expression of MHC in response to other stimulants such as lEN-y. 

In general, a liquid membrane for chiral separation contains an enantiospecific carrier which selectively forms a complex with one of the enantiomers of a racemic mixture at the feed side, and transports it across the membrane, where it is released into the receptor phase (Fig. 5-1). 

The carrier should not dissolve in the feed liquid or receptor phase in order to avoid leakage from the liquid membrane. In order to achieve sufficient selectivity, minimization of nonselective transport through the bulk of the membrane liquid is required. Liquid membranes can be divided into three basic types [6] emulsion supported and bulk liquid membranes, respectively (Fig. 5-2). 

FIGURE 2.16 Effects of successive rectangular hyperbolae on receptor stimulus, (a) Stimulus to three agonists, (b) Three rectangular hyperbolic stimulus-response functions in series. Function 1 ((3 = 0.1) feeds function 2 ((3 = 0.03), which in turn feeds function 3 ((3 = 0.1). (c) Output from function 1. (d) Output from function 2 (functions 1 and 2 in series), (e) Final response output from function 3 (all three functions in series). Note how all three are full agonists when observed as final response. 

Apelins and the Apelin Receptor. Figure 3 Scheme illustrating the hypothesised mechanisms of control of human (a) vasculartone and (b) cardiac contractility by apelin peptides ( ). In the vasculature, apelins (released via the small vesicles of the constitutive pathway) may act directly to activate apelin receptors on the underlying smooth muscle to produce vasoconstriction. This response may be modified by apelin peptides feeding back onto apelin receptors on endothelial cells to stimulate the release of dilators, such as nitric oxide. In heart, apelin peptides, released from endocardial endothelial cells, activate apelin receptors on cardiomyocytes to elicit positive inotropic actions. 

A receptor on nerve endings within a synapse that responds to the released neurotransmitter from that neuron. This then feeds back to the same neuron and negatively regulates the synthesis and release of that neurotransmitter. 

The cytokine leptin is secreted by adipocytes (fat cells) in proportion to the size of the adipose dq>ot and circulates via the bloodstream to the brain, where it ultimately affects feeding behavior, endocrine systems including reproductive function and, at least in rodents, energy expenditure. The major effect of Lqrtin is on the hy-pothalamous, where it suppresses appetite and hence food intake. Leptin exerts its effects via binding to the leptin receptor in the brain (specifically in the hypothalamus), which activates the JAK-STAT Pathway. 

Melanin-concentrating hormone (MCH) is a cyclic neuropeptide of 19 amino acids. It is involved in the modulation of feeding behavior. Its actions are mediated by G-protein coupled receptors (MCH1 and MCH2). 

The diffuse nature of orexinergic projections is consistent with combined patterns of expression of the two orexin receptors, which is widespread but differential and often complementary within and even outside the CNS. OX2Rs are found primarily in structures attributed to control of sleq)-wake functions, whereas OXIRs are more abundant in limbic structures controlling aspects of feeding, autonomic outflow, energy homeostasis, and to a lesser extent also REM-sleq). 

The neuropeptide Y (NPY) belongs to a family of peptides that includes peptide YY and pancreatic polypeptide, and it is associated with several diseases such as asthma, immune system disorders, inflammatory diseases, anxiety, depression and diabetes mellitus. NPY is found in the central and peripheral nervous system, and its biological functions are mediated by interactions with five receptor sub-types, i.e. Yl, Y2, Y4, Y5 and Y6. Several studies indicate that the feeding behavior is influenced by interactions between NPY and Yl and Y5. Deswal and Roy used Cerius descriptors and genetic function approximation QSAR to investigate the structural determinants for the inhibition potency of 24 compounds with the general structure 4 for the NPY Y5 receptor [31]. The best QSAR (H = 0.720,... 

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