Molecular cloning and characterization of a new human histamine receptor, HH4R

Molecular cloning and characterization of a new human histamine receptor, HH4R
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一种新的人类组胺受体 HH4R 的分子克隆和表征

DOI:
10.1006/bbrc.2000.4008
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发表时间:
2000-12-20
影响因子:
3.1
通讯作者:
Tanaka, K
Tanaka, K
中科院分区:
生物学4区
文献类型:
--
作者:
Nakamura, T;Itadani, H;Tanaka, K

文献摘要

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从人白细胞cDNA中克隆了一个新的组胺受体HH 4 R。推导的氨基酸序列与人组胺H3受体HH 3R的氨基酸序列同源性约为40%。表达HH 4 R的细胞对组胺有反应,抑制毛喉素诱导的cAMP积累。H3激动剂N-α-甲基组胺(NAMHA)特异性结合HH 4 R,而另一种H3激动剂R(-)-α-甲基组胺(RAMHA)和H3拮抗剂硫代哌丁胺则与这种结合竞争。RAMHA,NAMHA,imetit抑制毛喉素诱导的cAMP在HH 4 R表达细胞中的积累。然而,H3激动剂对HH 4 R的结合亲和力和激动活性弱于对HH 3R的结合亲和力和激动活性。通过RT-PCR在多种外周组织中检测到HH 4 R的低表达;然而,与HH 3R相反,在脑中未检测到表达。这些观察结果表明,克隆是一个不同的组胺受体从HH 3R,因此被命名为HH 4 R。(C)北京大学出版社.
A new histamine receptor, HH4R, was cloned from human leukocyte cDNA. The deduced amino acid sequence showed about 40% identity to that of the human histamine H3 receptor, HH3R. HH4R-expressing cells responded to histamine, inhibiting forskolin-induced cAMP accumulation. An H3 agonist, N-alpha -methylhistamine (NAMHA), bound specifically to HH4R, while another H3 agonist, R(-)-alpha -methylhistamine (RAMHA), and the H3 antagonist, thioperamide, competed with this binding. RAMHA,NAMHA, and imetit inhibited forskolin-induced cAMP accumulation in HH4R-expressing cells. However, the binding affinities and agonistic activities of H3 agonists to HH4R were weaker than those to HH3R Low expression of HH4R was detected in a wide variety of peripheral tissues by RT-PCR; however, in contrast with HH3R, expression was not detected in the brain. These observations indicate that the clone is a distinct histamine receptor from HH3R, and thus is named HH4R. (C) 2000 Academic Press.