Receptors, effect

FIGURE 9.18 Multiple receptor effects (ordinates denote pK values for antagonism or receptor occupancy) of (a) yohimbine and (b) amitriptyline. 

Hormones, peptides and neurotransmitters Effect of ICV injection on food intake Effect of gene deletion on food intake Response to adiposity signals Receptor Effect of receptor defect on food intake... 

It is easy to speculate that in an active neuron with a rapid firing pattern, the continued release of a peptide may eventually lead to depletion of the peptide occurring. This has been shown in the peripheral nervous system. If this also happens in the CNS it would provide a mechanism whereby the release and resultant receptor effects of a transmitter no longer match the firing pattern and demands of the neuron and so could contribute to long-term adaptations of neurons by a reduction in the time over which a peptide is effective. 

Viel, G.T., Yang, Q., Lundahl, P, Ensing, K., and de Zeeuw, R. A., Size-exclusion chromatographic reconstitution of the bovine brain benzodiazepine receptor. Effects of lipid environment on the binding characteristics, /. Chromatogr. A, 776, 101, 1997... 

Elner, VM, 2002. Retinal pigment epithelial acid lipase activity and lipoprotein receptors Effects of dietary omega-3 fatty acids. Trans Am Ophthalmol Soc 100, 301-338. 

A cardinal role for IL-4 in host protection against intestinal nematode infection was first shown in the H. polygyrus challenge model. Worm expulsion was delayed following treatment with anti-IL-4 or anti-IL-4 receptor monoclonal antibodies, while control treated animals successfully cleared infection (Urban et al., 1991b). Blockade of the IL-4 receptor effectively prevents the in vivo function of IL-4 and IL-13, as these two cytokines share the IL-4 receptor a-chain for signalling functions (Lin et al, 1995). In... 

Transmitter Transmitter parameter Receptor Effect Histamine parameter Receptor Effect... 

Fan, G.-F., Ray, K., Zhao, X., Goldsmith, R K and Spiegel, A. M. (1998) Mutational analysis of the cysteines in the extracellular domian of the human Ca2+ receptor effects on cell surface expression, dimerization and signal transduction. FEBSLett. 436, 353-356. 

Scheer, A., Costa, T., Fanelli, F., et al. (2000) Mutational analysis of the highly conserved arginine within the Glu/Asp-Arg-Tyr motif of the alpha) lb)-adrenergic receptor effects on receptor isomerization and activation. Mol. Pharmacol. 57,219-231. 

Escape behavior, effects of LSD and other hallucinogens on, 79-80 Excitatory 5-HT receptors effects of hallucinogens on activity of, 55-56... 

There is no simple or correct way to examine the causes of neurotoxicity. I have divided them into three overlapping areas neurotransmitter/receptor effects, which are often transient damage to the peripheral nerves, which is often permanent and damage to the developing nervous system, which is almost always permanent. 

Metman LV, DelDotto P, LePoole K, etal (1999) Amantadine for levodopa-induced dyskinesias—a 1-year follow-up study. Arch Neurol 56 1383-1386 Mirshahi T, Woodward JJ (1995) Ethanol sensitivity of heteromeric NMDA receptors effects of subunit assembly, glycine and NMDA receptorl mg2+-insensitive mutants. Neuropharmacology 34 347-355... 

Catalano M, Bellodi L, Lucca A, et al Lithium and alpha-2-adrenergic receptors effects of lithium ion on clonidine-induced growth hormone release. Neuroendocrinology Letters 6 61-66, 1984... 

The commonly used classes of antidepressants are discussed in the following sections, and information about doses and half-lives is summarized in Table 2-1. The antidepressant classes are based on similarity of receptor effects and side effects. All are effective against depression when administered in therapeutic doses. The choice of antidepressant medication is based on the patient s psychiatric symptoms, his or her history of treatment response, family members history of response, medication side-effect profiles, and comorbid disorders (Tables 2-2 and 2-3). In general, SSRIs and the other newer antidepressants are better tolerated and safer than TCAs and MAOIs, although many patients benefit from treatment with these older drugs. In the following sections, clinically relevant information is presented for the antidepressant medication classes individually, and the pharmacological treatment of depression is also discussed. The use of antidepressants to treat anxiety disorders is addressed in Chapter 3. 

Dopamine synthesis inhibitors interfere with the enzymes involved, and are identical to those discussed in section 4.3.5 (e.g., a-methyltyrosine (4.74), a tyrosine hydroxylase inhibitor). In this case, aj-adrenergic receptor effects are irrelevant, and only the classical competitive inhibitory effect is of any consequence. 

F. M. Cuss (1999). Beyond the histamine receptor effects of antihistamines on mast cells. Clin. 

Have some amine uptake inhibition but also antagonise Mianserin one or more of 5-HT2, ol-NA, o2-NA receptors. These Mirtazapine receptor effects increase amine availability in the synapse Nefazodone... 

However, there are now a number of second-generation (often caiied atypicaiO antipsychotics which have much reduced propensity to induce EPSEs. Most have a narrower spectrum of other receptor effects and a high ratio of 5-HT2 to D2 receptor antagonism. These drugs aii differ from each other in chemicai structure. 

Five key features of neurotransmitter function provide potential targets for pharmacologic therapy synthesis, storage, release, and termination of action of the transmitter, and receptor effects. These processes are discussed here in detail. 

Most of the direct organ system effects of muscarinic cholinoceptor stimulants are readily predicted from a knowledge of the effects of parasympathetic nerve stimulation (see Table 6-3) and the distribution of muscarinic receptors. Effects of a typical agent such as acetylcholine are listed in Table 7-3. The effects of nicotinic agonists are similarly predictable from a knowledge of the physiology of the autonomic ganglia and skeletal muscle motor end plate. 

Certain Hi antagonists, eg, cetirizine, inhibit mast cell release of histamine and some other mediators of inflammation. This action is not due to H -receptor blockade and may reflect an H4-receptor effect (see below). The mechanism is not fully understood but could play a role in the beneficial effects of these drugs in the treatment of allergies such as rhinitis. A few H4 antagonists (eg, terfenadine, acrivastine) have been shown to inhibit the P-glycoprotein transporter found in cancer cells, the epithelium of the gut, and the capillaries of the brain. The significance of this effect is not known. 

Sumatriptan Partial agonist at 5-HT1B/1D receptors Effects not fully understood may reduce release of calcitoningene-related peptide and perivascular edema in cerebral circulation Migraine and cluster headache Oral, nasal, parenteral duration 2 h Toxicity Paresthesias, dizziness, coronary vasoconstriction Interactions Additive with other vasoconstrictors... 

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