Human ADORA1/CHO
CBP71347
I. Background | |
ADORA1 是腺苷作用的 G 蛋白偶聯(lián)受體(Gi/o 型),廣泛分布于中樞神經(jīng)系統(tǒng)(海 馬、皮層)、心臟、腎臟及脂肪組織。其激活后通過 Gi 蛋白抑制腺苷酸環(huán)化酶(AC), 降低胞內(nèi) cAMP 水平并抑制 PKA 活性,同時(shí)促進(jìn) Gβγ 亞基開放鉀通道(如 GIRK) 并關(guān) 閉電壓門控鈣通道,導(dǎo)致神經(jīng)元超極化、神經(jīng)遞質(zhì)釋放減少(如谷氨酸),從而發(fā)揮神經(jīng) 抑制、抗驚厥、鎮(zhèn)痛及心肌負(fù)性變時(shí)作用。在病理狀態(tài)下,ADORA1 的過度激活可引發(fā)心 動(dòng)過緩或低血壓,而受體功能不足則與癲癇、神經(jīng)性疼痛及代謝紊亂相關(guān),成為治療神經(jīng) 系統(tǒng)疾病與心衰的潛力靶點(diǎn)。 |
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II. Description | |
cAMP 在 G 蛋白偶聯(lián)受體(GPCR)信號(hào)轉(zhuǎn)導(dǎo)中是一種關(guān)鍵的第二信使。當(dāng)配體結(jié)合到 GPCR,構(gòu)象發(fā)生變化,激活受體接著激活 G 蛋白,Gi 的激活導(dǎo)致腺苷酸環(huán)化酶調(diào)控 cAMP 的下調(diào)。
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III. Introduction | |
Host Cell: |
CHO |
Stability: | 20 passages (in-house test, that not means the cell line will be instable beyond the passages we tested.) |
Freeze Medium: | 90% FBS+10% DMSO |
Culture Medium: | F12K+10%FBS+5 μg/ml Puromycin |
Mycoplasma Status: | Negative |
Storage: | Liquid nitrogen immediately upon delivery |
Application(s): |
Functional assay for A1 receptor |
Transducer: | Gi |
IV. Description of Host Cell Line | |
Organism: | Hamster |
Tissue: | Ovary |
Morphology: | Epithelial |
Growth Properties: | Adherent |
V. Representative Data | |
Figure 2. HTRF cAMP Assay with ADORA1 CHO(C5). |