Download 5-HT4 Receptors in the Brain and Periphery by Robin D. Clark (auth.), Richard M. Eglen Ph.D. (eds.) PDF

By Robin D. Clark (auth.), Richard M. Eglen Ph.D. (eds.)

This e-book presents a complete, updated evaluate of the distribution, pharmacology and body structure of critical 5-hydroxytryptamine (5-HT)4 receptors. The 5-HT receptor subtypes express a special pharmacology, distribution and serve as, of which the 5-HT4 receptor has been the most intensively studied lately, either from a simple study perspective and as a goal for novel therapeutics.

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62. Romanelli MN, Ghelardini C, Die S et al. 1]oct-3-yl ester. Arzneim-Forsch/Drug Res 1993; 43:913-918. 63. Ramirez MJ, Garcia-Garayoa E, Monge A. VB2oB7, a novel 5-HTergic agent with gastrokinetic activity. I. Interaction with 5-HT3 and 5-HT4 receptors. J Pharm Pharmacol1997; 49:58-65. 64. Gaster LM, Sanger GJ. SB 204070: 5-HT4 receptor antagonists and their potential therapeutic utility. Drugs of the Future 1994; 19:1109-1121. 65. Gaster LM. 8th RSC-SCI medicinal chemistry symposium. Cambridge.

Both 5- HT45 and 5- HT41 receptors display a potential N glycosylation site in their amino terminus, and a potential palmitoylation site at the cysteine 329. Many G-protein-coupled receptors have a cysteine in the same position. >35•40 •44•47 Analysis of dendrograms (Fig. 3) by similarity analysis revealed a weak clustering of the 5- HT 4 receptor with the 5- HT2 subfamily. Comparison of the rat 5-HT4 sequence was as follows: rat 5-HT1A (7oo/o similarity), 5 rat 5-HT1n (67% similarity), 26 rat 5-HT1s (69% similarity)/ human 5-HT1E (69% similarity),55 rat 5-HT1p (68% similarity),34 rat 5-HT 2A (73% Fig.

C $ ':" K Y !. R. "::> ). :"... ' :.. C: 0 ':' V 1> C $ ':' ':' ":' : ~ C S ':' K Y :.. R 't ':' V :. Y. S C 0 M 0 ~ :. 2: X :. ! X S :> ? E S :. tr:"" t ~ ~ 1 Q 0 s: :I :. r. 0 :::: C' ~ t. T. ~ :;. S-M':'... c. cS-K':",,. o~-tr.. ):. Fig. 2. Alignment of amino acid sequences of the available 5-HT4 receptors. Differences in the human sequences are marked in gray. 48 Cloning of 5- HT4 Receptors from Other Species More recendy, the mouse 5-HT4L receptor has been cloned from cultured collicular neurons13 using PCR amplification.

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