Spadin 是一种从血液中释放的前肽衍生的天然肽，是一种有效的TREK-1 通道阻滞剂，其IC50值为 10 nM。Spadin 增强小鼠中缝背核 5-HT 神经传递，诱导海马 CREB 激活和神经发生。Spadin 可用于抗抑郁研究。
| 生物活性 | Spadin, a natural peptide derived from a propeptide released in blood, is a potentTREK-1 channelblocker withIC50value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research[1][2]. |
体外研究
(In Vitro) | Spadin (100 nM; COS-7 cells) has inhibitory effect of spadin on the TREK-1 channel and blocks 63% of the TREK-1 current stimulated by arachidonic acid[1].
Spadin (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice[1].
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体内研究
(In Vivo) | Spadin (10 μM; i.p.; for 30 min; male C57Bl/6J and TREK-1 deficient mice) increases of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN)[2].
Spadin (0.01-100 μM; ICV, i.p. and i.v.; daily, for 7 days; male C57Bl/6J and TREK-1 deficient mice) has anti-depressant behavior in mice[2].
| Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | | Dosage: | 10 μM | | Administration: | Intraperitoneal injection; for 30 min | | Result: | Increased of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN). |
| Animal Model: | Male C57Bl/6J and TREK-1 deficient mice[2] | | Dosage: | 0.01-100 μM | | Administration: | Intracerebroventrical injection, intraperitoneal injection and intravenous injection; daily, for 7 days | | Result: | Had any effect on mouse locomotion analyzed in short- or long-time after the drug injection. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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