1. Signaling Pathways
  2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)

Trace Amine-associated Receptor (TAAR) (痕量胺相关受体)

Trace amine associated-receptors (TAARs) are a class of G protein-coupled receptors that were discovered in 2001. Humans possess six functional isoforms (TAAR1, TAAR2, TAAR5, TAAR6, TAAR8, and TAAR9), whereas some fish species express over 100. It acts as an endogenous receptor for the trace amines. Trace amines are endogenous compounds classically regarded as comprising β-phenylethyalmine, p-tyramine, tryptamine, p-octopamine, and some of their metabolites.

Although all other TAARs serve predominantly or exclusively as chemosensory receptors in the main olfactory system, TAAR 1 has been demonstrated to be a novel modulator of dopaminergic, serotonergic and glutamatergic activity in the brain. And TAAR 1 has been identified as a novel therapeutic target for schizophrenia, depression, and addiction. In the periphery, TAAR1 regulates nutrient-induced hormone secretion, suggesting its potential as a novel therapeutic target for diabetes and obesity. TAAR1 may also regulate immune responses by regulating leukocyte differentiation and activation.

Trace Amine-associated Receptor (TAAR) 相关产品 (11):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110098
    Ro 5212773 99.85%
    Ro 5212773 (EPPTB) 是一种有效和选择性的 (TAAR1) 拮抗剂(对于小鼠 TAAR1 的 Ki 值为 0.9 nM),对其他 TAARs 没有显著影响。TAAR1 是一种 G 蛋白偶联受体 (GPCR),由内源性氨基酸代谢产物非选择性激活。
    Ro 5212773
  • HY-12700
    RO5256390 98.75%
    RO5256390 是口服有效的微量胺相关受体 1 (TAAR1) 的激动剂。RO5256390 在啮齿动物和灵长类动物模型中表现出促认知和抗抑郁样特性,显示出与 Olanzapine (HY-14541) 处理相似的大脑激活模式。RO5256390 能够阻断大鼠强迫性暴饮暴食行为。RO5256390 可抑制小鼠骨髓源性巨噬细胞中 ATP (HY-B2176) 诱导的 TNF 分泌。
    RO5256390
  • HY-12699
    RO5166017 99.48%
    RO5166017 是具有口服活性的、跨物种的 TAAR1 的激动剂,其对小鼠、大鼠、人和食蟹猴的 Ki 值分别为1.9 nM、2.7 nM、31 nM 和 24 nM。
    RO5166017
  • HY-109157
    Ralmitaront Agonist 99.92%
    Ralmitaront (RO6889450) 是一种具有口服活性的微量胺相关受体 1 (TAAR1) 的激动剂,EC50 值为 110.4 nM。Ralmitaront 在啮齿动物中具有抗精神病、认知改善和抗抑郁的活性。Ralmitaront 可作为一种神经抑制剂,用于神经相关疾病的研究,如精神分裂症 (SCZ)、分裂情感性障碍。
    Ralmitaront
  • HY-108015
    RO5263397 98.87%
    RO5263397 是一种有效的,选择性的和口服的 TAAR1 激动剂,对人TAAR1 和大鼠 TAAR1 的 EC50 分别为 17 和 35 nM。RO5263397调节清醒度和 EEG 频谱组成。
    RO5263397
  • HY-W909149
    TAAR1 agonist 3 Agonist
    TAAR1 agonist 3 是一种微量胺相关受体1 (TAAR1) 激动剂 (pEC50=7.6)。TAAR1 agonist 3 也是 α2AR 的完全激动剂 (pEC50= 6)。TAAR1 agonist 3 可用于神经精神疾病的研究。
    TAAR1 agonist 3
  • HY-W909173
    TAAR1 agonist 2 Agonist
    TAAR1 agonist 2 (compound 30) 是一种微量胺相关受体1 (TAAR1) 的完全激动剂 (pEC50=7.5)。TAAR1 agonist 2 在 H1 受体上也表现出激动剂活性,并激活了毒蕈碱乙酰胆碱受体家族的几个成员,例如 M2 受体 (pEC50=5)。TAAR1 agonist 2 可用于神经精神疾病的研究。
    TAAR1 agonist 2
  • HY-42346
    ZH8651

    4-溴苯乙胺 1G

    Agonist 99.71%
    ZH8651 是 TAAR1 的激动剂,可同时激活 Gs 和 Gq 信号通路。ZH8651 可用于研究精神分裂症。
    ZH8651
  • HY-161317
    Gαq/11 protein-IN-1 Agonist
    Gαq/11 protein-IN-1 (compound F33) 是一种 Gαq/11 蛋白抑制剂,IC50 值为 9.4 μM。 Gαq/11 protein-IN-1 具有抗肿瘤活性。
    Gαq/11 protein-IN-1
  • HY-157955
    TAAR1 agonist 1 Agonist
    TAAR1 agonist 1 (compound 6E) 是一种有效的 TAAR1 激动剂,具有有效的 TAAR1-Gs/Gq 双通路激活特性。TAAR1 agonist 1 显着缓解 MK-801 诱导的精神分裂症样认知表型。
    TAAR1 agonist 1
  • HY-157955A
    TAAR1 agonist 1 hydrochloride Agonist
    TAAR1 agonist 1 hydrochloride (6e·HCl) 是一种新型的 G 蛋白偶联受体 TAAR1 激动剂。TAAR1 agonist 1 hydrochloride 可用于精神分裂症的研究。
    TAAR1 agonist 1 hydrochloride