Cloning, expression and pharmacology of the mouse 5-HT4L receptor

被引：60

作者：

Claeysen, S ^{[1
]}

Sebben, M ^{[1
]}

Journot, L ^{[1
]}

Bockaert, J ^{[1
]}

Dumuis, A ^{[1
]}

机构：

[1] CTR PHARMACOL ENDOCRINOL,CNRS UPR 9023,INSERM,F-34094 MONTPELLIER 05,FRANCE

来源：

FEBS LETTERS | 1996年 / 398卷 / 01期

关键词：

mouse colliculi; 5-HT4; receptor; cloning; distribution; splice variant;

D O I：

10.1016/S0014-5793(96)01132-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Since most of our knowledge on pharmacological properties of brain 5-HT4 receptors have been discussed for mouse colliculi neurons, we cloned the corresponding receptor using the RT-PCR approach. As expected, the homology with the already cloned rat 5-HT4L receptor was high, revealing only 16 differences at the amino-acid level. One of the differences, proline(75) in mouse, alanine(75) in the already published rat sequences was not confirmed. Therefore this proline is part of the consensus sequence present in all 5-HT receptor transmembrane domain II (LVMP). Comparing the affinities of 11 agonists and five antagonists for the cloned mouse receptor (5-HT4L) expressed in LLCPK1 and the corresponding receptor in mouse colliculi shows an excellent correlation. The transfected mouse 5-HT4L receptor stimulated cAMP production, When expressed at high density, it exhibited intrinsic activity, In contrast to the previously described distribution, we found that mRNA encoding for both the short (5-HT4S) and the long form (5-HT4L) of 5-HT4 receptors are expressed in all mouse and rat brain areas.

引用

页码：19 / 25

页数：7

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