Labeling Receptors

Largent, B.L. Gundlach, A.L. and Snyder, S.H. Psychotomimetic opiate receptors labeled and visualized with (+)-3H-3-(3-hydroxyphenyl)-N-(l-propyl Ipiperidine. Proc Natl Acad Sci USA 81 4983-4987, 1984. 

Yet, cyclazocine was able to displace the binding of 3H-PCP. These findings are consistent with the finding that metaphit can only bind irreversibly to about 50 percent of the receptors labeled by 3H-PCP (Rafferty et al. 1985), which indicates that 3H-PCP binds to more than one type of receptor. Thus, PCP and cyclazocine probably exert their effects through different receptors. 

FIGURE 14-5 Isoforms of the rat H3 receptor. The genomic structure of the receptor (top) shows four exons (boxes, E1-E4) and three introns (bp sizes are in parentheses). Peptide sequences that correspond to translated TM regions are labeled with roman numerals (I—VII). An alternatively spliced region (orange box) is depicted between the stop sequences. Six isoforms of the receptor (labels are on the left) result from alternative splicing. (Modified with permission from reference [2].)... 

Sinkins, W. G., Kandel, M Kandel, S. I., Schunack, W and Wells, J. W. (1993) G protein-linked receptors labeled by [3H]histamine in guinea pig cerebral cortex. I. Pharmacological characterization [corrected]. Mol. Pharmacol. 43, 583-594. 

In vivo receptor labeling offers binding conditions similar to those prevailing in the physiological state and it provides anatomical resolutions compatible with perfusion fixation of target tissue. This technique is... 

Bouchard P, Roman F, Junien JL, Quirion R. 1996. Autoradiographic evidence for the modulation of in vivo sigma receptor labeling by neuropeptide Y and calcitonin gene-related peptide in the mouse brain. J Pharmacol Exp Ther 276 223-230. 

Schwartz RD, McGee R Jr, Kellar KJ (1982) Nicotinic cholinergic receptors labeled by [ H]acetylchohne in rat brain. Mol Pharmacol 22 56-62... 

A gastrinlike neuropeptide, CCK exists in the central nervous system both as an octapeptide [CCK-8] and as a tetrapeptide (CCK-4) (Rex et al. 1994b). The octapeptide CCK-8 occurs predominantly in sulfated form and is one of the most abundant neuropeptides in the central nervous system (Rex et al. 1994b]. Two major subtypes of CCK receptors, labeled as CCK-A and CCK-B receptors, have been identified (Hill et al. 1993]. At this point, the most promising neuropeptide receptor to target for the treatment of anxiety may be the CCK-B receptor. This receptor is widely distributed throughout... 

Schwartz RD, Lehmann J, Kellar KJ Presynaptic nicotinic cholinergic receptors labeled by [3H]acetylcholine on catecholamine and serotonin receptors in brain. J Neurochem 42 1495-1498, 1984... 

Sorba, G. Tertuik, W. Ganellin, C. R. Synthesis and authentication of iodoazidophenpyr-amine, a photoaffmity reporter ligand previously used for histamine Hj-receptor labelling. Arch. Pharm. (Weinheim) 1995, 328, 677-680. 

Spier AD, Wotherspoon G, Nayak SV, Nichols RA, Priestley JV, Lummis SC. Antibodies against the extracellular domain of the 5-HT3 receptor label both native and recombinant receptors. Brain Res Mol Brain Res 1999 67 221-230. 

Fig. 8. 5-HT4 receptors in the human and monkey brain. Autoradiographic visualization of 5-HT4 receptors labelled with 0.02 n / [125I]SB 207710 in several regions of the...

Naudon L, El Yacoubi M, Vaugeois JM, Leroux-Nicollet I, Costentin J. A chronic treatment with fluoxetine decreases 5-HT(lA) receptors labeling in mice selected as a genetic model of helplessness. Brain Res 2002 936(l-2) 68-75. 

Fig. 3. Cross-linking of l25I-labelled human GH to rabbit liver receptors. Labelled GH was incubated with receptors, cross-linked with disuccinimidyl suberate and then subjected to SDS polyacrylamide gel electrophoresis. 1. Total binding 2-4. Displacement with 1 fig unlabelled human GH, bovine GH and ovine prolactin respectively 5. l25I-human GH without receptors. Note the major GH-receptor complex of M, = 80000 (indicating a receptor protein or subunit of Af, 58000) and various other components of larger and smaller M,.

Dopamine receptor labeling in terminals presynaptic to asymmetrical synapses... 

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