Receptor characterization

The most frequent posttranslational modifications for GPCRs are N-glycosylation at the N-terminus and external loop Asn-X-Ser/Thr sequences (human calcitonin receptor-like receptor [61] and un,-adrenergic receptor [62]), pabnitoylation (human dopamine Di receptor [63]), and phosphorylation ( 2 adrenergic receptor [64]). 

For many receptors different subtypes with a high degree of sequence homology are known. In cases such as the neuropeptide Y receptor family - with the Yj, Y2, Y4, and Y5 receptors functionally expressed in humans - or the angiotensin II receptor family - with the receptors AT,/., A l i. and AT2 in human - antibodies that distinguish between different receptor subtypes are a valuable tool to monitor the receptor expression on the protein level [48, 49]. 

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The largest numbers of integrins are members of the (31 integrins, also known as the very late antigen (VLA) subfamily because of its late appearance after activation. There are at least seven receptors characterized from this subfamily, each with different ligand specificity. Among the most studied include the 04(31 and a5 31 receptors. The leukocyte integrin a4 31 is a cell adhesion receptor that is predominantly expressed on lymphocytes, monocytes and eosinophils. 

Hoyer D, Epelbaum J, Feniuk W, Humphrey PPA, Meyerhof W, O caroll AM, Patel Y, Reisine T, Reubi JC, Schindler M, Schonbmnn A, Taylor JOB, Vezzani A (2000) Somatostatin receptors. In Watson SP, Girdlestone D, ed. The IUPHAR compendium of Receptor Characterization and Classification, 2nd edn., pp. 354—364. London IUPHAR Media... 

ZuKin, S.R. Tempel, A. Gardner, E.L. and Zukin, R.S. Interaction of 3H(-)SKF-10,047 with brain sigma opioid receptors Characterization and autoradiographic visualization. Submitted for publication. 

Caulfield, M. P. (1993). Muscarinic receptors - characterization, coupling and function. Pharmacol. Ther. 58, 319-79. 

In ed. IUPHAR, The IUPHAR Compendium of Receptor Characterization and Classification, 2nd Edition. (London IUPHAR Media) pp. 271-7. 

Knoflach, F., Mutel, V., Jolidon, S., et al. (2001) Positive allosteric modulators of metabotropic glutamate 1 receptor characterization, mechanism of action, and binding site. Five. Natl. Acad. Sci. USA 98,13402-13407. 

Adkins, C. E., Pillai, G. V., Kerby, J., et al. (2001) alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential. J. Biol. Chem. 276, 38934-38939. 

Electrical stimulation in the vicinity of the raphe nuclei has been reported to produce depressant effects on MSRs (32,142). These depressant effects could be attributed to activation of postsynaptic inhibitory receptors analogous to those characterized in the forebrain, except for the fact that the depression was blocked by 5-HT antagonists. The effectiveness of the antagonists suggests that the receptor is more akin to the excitatory 5-HT receptor characterized on motoneurons (134,184). The depressant behavioral effects could result from... 

Poland A, Teitelbaum P, Glover E. 1989. [1251]2-lodo-3,7,8-trichlorodibenzo-p-dioxin-binding species in mouse liver induced by agonists for the Ah receptor Characterization and identification. Mol Pharmacol 36(1 ) 113-120. 

The evidence to-date shows that vertebrate photoreception is mediated by a closely related group of proteins termed opsins. These are G protein-coupled receptors characterized by their ability to bind a vitamin A based chromophore ( -cis-retinal) via a Schiff base linkage using a lysine residue in the 7th transmembrane a helix (Fig. 1). The primary events of image detection by the rods and cones occurs with the absorption of a photon of light by ll-r/r-retinal and its photoisomerization to the AUtrans state (Bums Baylor 2001, Menon et al 2001). Although photoreception is best understood in retinal rods and cones, photoreception is not confined to these structures. In non-mammalian... 

K.-H. Ruan, J. Wu, S.-P. So, L.A. Jenkins, Evidence of the residues involved in ligand recognition in the second extracellular loop of the prostacyclin receptor characterized by high resolution 2D NMR techniques. Arch. Biochem. Biophys. 418 (2003) 25. 

Waller CL McKinney JD (1995) Three-dimensional quantitative structure activity relationships of dioxins and dioxin-like compounds Model validation and Ah receptor characterization. Chem Res Toxicol, 8 847-858. 

Novick D, Cohen B, Rubinstein M. The human interferon oc/(3 receptor characterization and molecular cloning. Cell 1994 77 391-400. 

Durand IH, Green RD (2001) Cloning of a chick A3 adenosine receptor characterization of ligand binding and receptor-effector coupling of chick A1 and A adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol 363(1) 81—89... 

The term "H3 receptor" has been coined by Arrang et al.1 H3 receptors are located on paracrine cells and on neurones activation of H3 receptors usually causes inhibition of the release of the respective mediator or neurotransmitter. The receptor characterized by Arrang et al.1 is an example of an autoreceptor, i.e. of a receptor via which the transmitter released from a given neurone influences its own release. H3 receptor-mediated inhibition of the release of transmitters other than histamine has also been described such receptors are known as heteroreceptors. The present review will focus on H3 heteroreceptors in the central nervous system (CNS) in separate chapters of this book, H3 autoreceptors, H3 heteroreceptors in the neuroendocrine system as well as H3 receptor-mediated modulation of transmitter release in vivo will be considered. A separate article will also deal with H3 heteroreceptors in peripheral tissues although an example of an H3 receptor in the retina will be covered in our chapter, due to the close relationship between CNS and retina2. 

Cumming, P., Shaw, C. and Vincent, S.R. (1991). High affinity histamine binding site is the H3-receptor - characterization and autoradiographic localization in rat brain. Synapse 8, 144-151. 

Results of Current Studies Involving Receptor Characterization... 

Rebola R, Oliveira CR, Cunha RA (2002) Transducing system operated by adenosine A2A receptors to facilitate acetylcholine release in the rat hippocampus. Eur J Pharmacol 454 31-8 Reddington M, Lee KS, Schubert P (1982) An Ai-adenosine receptor, characterized by [3H] cy-clohexyladenosine binding, mediates the depression of evoked potentials in a rat hippocampal slice preparation. Neurosci Lett 28 275-9... 

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