多巴胺受體D二
多巴胺受體 D 二(Dopamine receptor D 二,簡稱D 二 R), 為著轉譯自 _ DRD 二 _ 基因的一種多巴胺受體卵白。D 二 R 上早佇一九七五年為 Philip Seeman 所發現講,並共號名做「抗精神疾患性多巴胺受體」(_ antipsychotic dopamine receptor _)。 D 二 R 為所有抗精神病藥物的作用標的。
功能
D 二 R 屬於一種多巴胺受體,並會佮 Gi 結合。Gi 為 G 卵白尪仔聯受體的一種亞型,會壓制腺酸環化扣的活性。
佇鳥鼠仔模式當中,齒型的轉來 neuronal calcium sensor 影一(NCS 影一)會影響 D 二 R 佇細胞膜的表現量。這項機制會影響雄雄有塑性佮記持形成。
佇胡蠅模式內底,多巴胺性神經元上的 D 二 R 自體受器能避免神經元死亡,進一步引發類帕金森症的症頭。
仝型體
Alternative splicing of this gene results in three transcript variants encoding different isoforms .
The long form (D 二 Lh) has the " canonical " sequence and functions as a classic post-synaptic receptor . The short form (D 二 Sh) is pre-synaptic and functions as an autoreceptor that regulates the levels of dopamine in the synaptic cleft . Agonism of D 二 sh receptors inhibits dopamine release ; antagonism increases dopaminergic release . A third D 二 ( Longer ) form differs from the canonical sequence where 兩百七十 V is replaced by VVQ .
基因組
等位基因變化:
- A 抹兩百四十一 G
- C 一百三十二 T、G 四仔二三 A、T 七仔六十五 C、C 九百三十九 T、C 九百五十七 T,以及 G 一千一百空一 A
- Cys 三百十一 Ser
- 抹一百四十一 C insertion / deletionThe polymorphisms have been investigated with respect to association with schizophrenia .
Some researchers have previously associated the polymorphism Taq 一 A ( rs 一百八十五空四百九十七 ) to the _ DRD 二 _ gene . However , the polymorphism resides in exon 八 of the _ ANKK 一 _ gene . DRD 二 TaqIA polymorphism has been reported to be associated with an increased risk for developing motor fluctuations but not hallucinations in Parkinson's disease .
配體
Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D 二 receptor , but are , in general , very unselective , at best selective only for the " D 二-like family " receptors and so binding to D 二 , D 三 and D 四 , and often also to many other receptors such as those for serotonin and histamine , resulting in a range of side-effects and making them poor agents for scientific research . In similar manner , older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another , and , although most of these agents do act as D 二 agonists , they affect other subtypes as well . Several selective D 二 ligands are , however , now available , and this number is likely to increase as further research progresses .
受體致活劑
部份受體致活劑
受體絚抗劑
異位調控因為
Functionally selective ligands
- 參見參考文獻。
Protein–protein interactions
The dopamine receptor D 二 has been shown to interact with EPB 四十一 L 一 , PPP 一 R 九 Band NCS 影一 .
Receptor oligomers
The D 二 receptor forms receptor heterodimers _ in vivo _ ( in living animals ) with other G protein-coupled receptors ; these include :
- D 一–D 二 dopamine receptor heteromer
- D 二–adenosine A 二 A
- D 二–ghrelin receptor
- D 二 sh–TAAR 一
The D 二 receptor has been shown to form hetorodimers _ in vitro _ ( and possibly _ in vivo _ ) with DRD 三 , DRD 五 , and 五-HT 二 A .
註解
參考文獻
外部連結
- 醫學主題詞表(MeSH): _ Receptors , + Dopamine + D 二 _
- Pappas , Stephanie . Study : Genes Influence Who Your Friends Are . Imaginova Corp . LiveScience . [二十 January 二千空一十一] .
多巴胺受體 D 二引用美國國家醫學圖書館提供的資料,遮的資料屬於公共領域。
Template : Dopaminergics