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PGlu-3-methyl-His-Pro-NH2 TFA

CAS No. :

MCE 站：PGlu-3-methyl-His-Pro-NH2 TFA

产品活性：PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA) 是一种修饰的促甲状腺激素释放激素 (TRH) 肽，能增强与垂体促甲状腺素释放激素受体的结合，增加垂体促甲状腺素 (TSH) 释放的刺激。PGlu-3-methyl-His-Pro-NH2 TFA 在增强剂乙醇和桉叶碱下，通过大鼠皮肤的体外通透性增加。

研究领域：Others

作用靶点：Others

In Vitro: PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA) has a very high affinity for the TRH receptor in the CNS. PGlu-3-methyl-His-Pro-NH2 TFA is more potent in eliciting behavioral effects as well as being more potent in the release of both growth hormone and thyroid stimulating hormone.

In Vivo: PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA) (300 μg/kg; i.v.) elicits a 80 % increase in cerebral blood flow. Even a minute dose of PGlu-3-methyl-His-Pro-NH2 TFA (625 ng kg-1) causes an increase in cerebral blood flow.
The addition of 3% terpene in combination with 47% ethanol increases the penetration of PGlu-3-methyl-His-Pro-NH2 TFA (5 mg/ml; transdermal administration; 30 minutes).
Topical application of PGlu-3-methyl-His-Pro-NH2 TFA induces an increase in TSH serum concentration from 0.32 ng/ml to 22.9 ng/ml, respectively, after 30 min. The addition of Terpene and Ethanol in combination with TRH or PGlu-3-methyl-His-Pro-NH2 TFA, increases the TSH release to 43 and 48.4 ng/ml, respectively.

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