2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. GR 64349 acetate

GR 64349 acetate 是选择性的神经激肽 2 (NK2) 受体激动剂。GR 64349 acetate 可选择性激活 NK-2 受体亚型。GR 64349 acetate 可激活排尿反射的强直性和节律性膀胱收缩。GR 64349 acetate 不会抑制生理盐水诱导的节律性膀胱收缩激活。GR 64349 acetate 可诱导内向电流。

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GR 64349 acetate

GR 64349 acetate Chemical Structure

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GR 64349 acetate 的其他形式现货产品:

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Other Forms of GR 64349 acetate:

GR 64349 acetate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GR 64349 acetate is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 acetate selectively activates the NK-2 receptor subtype. GR 64349 acetate activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 acetate induces inward currents[1][2].

IC50 & Target[1]

NK2R

 

体外研究
(In Vitro)

GR 64349 可在体外收缩分离的大鼠膀胱组织，其效力与选择性 NK-1 激动剂 GR 73632 相当[1]。
GR 64349 (300-500 nM) 在部分神经元中产生了内向电流[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GR 64349 acetate 相关抗体:
体内研究
(In Vivo)

GR 64349 (0.1-10 nmoles/kg；动脉注射) acetate 作用于外周 NK-2 受体，可剂量依赖性地提高乌拉坦麻醉大鼠的膀胱强直性收缩水平并激活膀胱节律性收缩，其中强直性收缩的 ED50 为 0.61 nmoles/kg i.a.，膀胱节律性收缩的 ED50 为 0.43 nmoles/kg i.a.[1]。
GR 64349 (侧脑室注射) acetate 不会调节氨基甲酸乙酯麻醉大鼠中中枢介导的膀胱节律性收缩[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar-Morini (male, 300-350 g, urethane-anesthetized, urinary bladder cannulated and filled to 0.25 mL saline)[1]
Dosage: 0.1 nmoles/kg; 1 nmoles/kg; 10 nmoles/kg
Administration: i.a.
Result: Induced a dose-related increase in intravesical pressure (tonic contraction, TC) and activation of rhythmic bladder contractions (RBC).
Reached maximal TC amplitude of 37 mmHg (n=6-7).
Achieved ED50 of 0.61 nmoles/kg i.a. for TC (95% confidence limits: 0.36-1.03).
Achieved ED50 of 0.43 nmoles/kg i.a. for RBC (95% confidence limits: 0.15-1.26).
Observed RBC in 4-6 out of 6 preparations at 1 nmoles/kg i.a.
Left TC largely unaffected after topical TTX pretreatment, which abolished RBC.
Showed maximal TC amplitudes of 28 mmHg (without antagonist) and 26 mmHg (with GR 82334 pretreatment, n=5), with GR 82334 not inhibiting GR 64349-induced TC.
分子量

981.17

Formula

C44H72N10O13S
Sequence

Lys-Asp-Ser-Phe-Val-{Aaa}-Leu-Met-NH2
Sequence Shortening

KDSFV{Aaa}LM-NH2
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.
纯度 & 产品资料
参考文献

GR 64349 acetate 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GR 64349GR64349GR-64349Neurokinin ReceptorNK receptorTachykinin receptorrat urinary bladder tissueneurokinin 2 (NK2) receptorNK-2 receptor subtypesmicturition reflexrat periaqueductal grey neuronsurethane-anesthetized ratsperipheral NK-2 receptorsInhibitorinhibitorinhibit

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