ニューロペプチドFF F-8-F-NH2
ニューロペプチドFF F-8-F-NH2 · ニューロペプチドFF · ノイロペプチドFF · F8Fアミド · (2S)-2-{[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-アミノ-3-フェニルプロパンアミド]-4-メチルペンタンアミド]-3-フェニルプロパンアミド]-4-カルバモイルブタノイル]ピロリジン-2-イル]ホルムアミド}-N-[(1S)-4-カルバムイミドアミド-1-{[(1S)-1-カルバモイル-2-フェニルエチル]カルバモイル}ブチル]ペンタンジアミド · NPFF · NPAF · ninamide
識別子と物理属性
| CAS No. | 99566-27-5 |
|---|---|
| 分子式 | C54H76N14O10 |
| 平均分子量 | 1,081.27 g/mol |
| SMILES | CC(C)C[C@H](NC(=O)C(N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NC(Cc1ccccc1)C(N)=O |
| InChIKey | HWYCFZUSOBOBIN-AQJXLSMYSA-N |
| PubChem CID | 123797 |
| 現地名 | ニューロペプチドFF F-8-F-NH2 |
化学・物理的性質
| 貯蔵条件 | −20°C |
|---|---|
| 溶解度 | Water: 1 mg/ml水に 0.50 mg/ml まで溶解します。 |
| 外観・状態 | Solid |
| 色 | White to off-white |
安全性と法規制
| 水環境危害等級（WGK） | 3 |
|---|
用途
説明
Neuropeptide FF (NPFF) is a peptide expressed in the brain and spinal cord that shares a precursor protein with neuropeptide AF. NPFF is expressed primarily in the posterior pituitary, hypothalamus, and medulla. It is an agonist at NPFF1 and NPFF2 receptors (Kis = 2.82 and 0.21 nM, respectively, for human recombinant receptors) that inhibits forskolin-induced cAMP production in CHO cells (EC50s = 236 and 2.3 nM, respectively). NPFF activates parvocellular neurons in the paraventricular nucleus (PVN) of the hypothalamus to stimulate oxytocin release from their projections in the brain stem, thereby regulating baroreflex control of heart rate. However, it inhibits magnocellular PVN neurons by enhancing GABAergic input. It is also found in plasma and exogenous administration briefly increases mean arterial pressure (MAP) by 40 mm Hg in rats, an effect that is only partially blocked by the norepinephrine competitor guanethidine and the α1-adrenergic receptor antagonist prazosin . NPFF has anti-opioid effects in rodent models, inhibiting morphine-induced analgesia and inducing abstinence in morphine-tolerant rats. It also inhibits acquisition of conditioned place preference to cocaine in rats when administered at doses of 10 and 20 nmol.
使用
Endogenous antiopioid peptide and agonist at NPFF1 and NPFF2 receptors (Ki values are 2.82 and 0.21 nM respectively). Exhibits anorexigenic effects.