Rotundine

製品コードS2437 バッチS243701

化学情報

	Synonyms	L-tetrahydropalmatine, L-THP	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₂₅NO₄
	分子量	355.43	CAS No.	483-14-7
Solubility (25°C)*	体外	DMSO	8 mg/mL (22.5 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
in vitro	Rotundine displays a higher affinity to dopamine D1 than D2 receptor with K_i of 124 nM and 388 nM, respectively, while the IC50 values are 166 nM (D1) and 1.47 μM (D2), respectively. Rotundine exhibits a weak inhibitory activity against dopamine D3 with IC50 of 3.25 μM. Rotundine also potently inhibits 5-HT1A with IC50 of 374 nM and K_i of 340 nM. In addition to the antagonism of postsynaptic dopamine receptors, inhibition of presynaptic autoreceptors by Rotundine leads to increased dopamine release, which is probably attributed to lower affinity of Rotundine for D2 receptors. Along with dopamine receptors, Rotundine can interact with a number of other receptor types, including α-1 adrenergic receptors, at which it functions as an antagonist, and γ-aminobutyric acid receptors, at which it facilitates γ-aminobutyric acid binding through positive allosteric effects. ^[1]
in vivo	Rotundine treatment does not affect the locomotor activity at the doses of 6.25 mg/kg, 12.5 mg/kg, or 18.75 mg/kg, but significantly antagonizes the hyperactivity induced by oxy-codone (5 mg/kg). ^[2] Oral administration of Rotundine (10-25 mg/kg) significantly increases hot-plate latency of mice, indicating that Rotundine exerts remarkable analgesic activity, which is associated with β-endorphin neurons in the arcute nucleus and supraspinal D2 receptor. ^[3] Administration of Rotundine (1-10 mg/kg) dose-dependently increases, while 20 mg/kg decreases the rate of cocaine self-administration under fixed-ratio (FR) reinforcement, due to a postsynaptic, rather than presynaptic, DA receptor blockade mechanism. In contrast to the effects on cocaine's actions, only the 10 mg/kg dose of Rotundine but not 1 mg/kg or 3 mg/kg produces inhibitory effect on sucrose self-administration and locomotion. ^[4] LD50: Mice 1160mg/kg (i.g.) ^[5]

プロトコル(参考用のみ)

動物実験	動物モデル	Female ICR mice subjected to hot plate latency assay
	投薬量	25 mg/kg
	投与方法	Oral administration

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

An antiviral drug screening system for enterovirus 71 based on an improved plaque assay: A potential high-throughput method [ J Med Virol, 2019, 91(8):1440-1447]	PubMed: 30900754

An antiviral drug screening system for enterovirus 71 based on an improved plaque assay: A potential high-throughput method [ J Med Virol, 2019, 91(8):1440-1447]

PubMed: 30900754

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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