Hemokinin 1 (mouse)

Hemokinin 1 (mouse) 是一种选择性的神经激肽-1 受体激动剂，对人 NK1 受体和人 NK2 受体的 Ki 分别为 0.175 nM 和 560 nM。

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货号: ajci10720
CAS: 208041-90-1
别名:
分子式: C61H100N22O15S
分子量: 1413.65
纯度: >98%
溶解度: Soluble to 2 mg/ml in sterile water
储存: Store at -20°C
库存: 现货

Background

Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with Ki of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.
Hemokinin 1 (mouse) (1?nM-3?μM) produces concentration-dependent contraction of RUB averaging 66±3% (n=6) of the maximal contraction produced by KCl (80?mM). Hemokinin 1 (mouse) (10?nM-10?μM) induces a quickly-developing contractile responses of GPI, as does the tachykinin NK3 receptor selective agonist senktide or neurokinin B (NKB). Hemokinin 1 (mouse) induces full agonist responses but with a 500 fold lower potency as compared to NKB[1].
Hemokinin 1 (mouse) (0.01-100?nmol/kg i.v., n=10) induces a dose-related hypotension that is maximal at the dose of 10?nmol/kg. For systolic blood pressure (SBP), the ED50 value is 0.2?nmol/kg (0.1-0.4?nmol/kg) for Hemokinin 1 (mouse). For diastolic blood pressure (DBP), the ED50 value is 0.1?nmol/kg (0.07-0.2?nmol/kg) for Hemokinin 1 (mouse). Hemokinin 1 (mouse) (0.1-100?nmol/kg, i.v.) induces a dose-related salivary secretion in atropine-pretreated rats[1].
Reference:
[1]. Francesca Bellucci, et al. Pharmacological profile of the novel mammalian tachykinin, hemokinin 1. Br J Pharmacol. 2002 Jan; 135(1): 266-274

Protocol

Animal experiment:

Male albino Wistar Rats weighing 400-450?g are used throughout the study. On the day of the experiment, rats are anaesthetized with urethane (1.2?g/kg, s.c.). Following tracheotomy and placement of a tracheal cannula (PE 205), the left jugular vein is cannulated (PE50) for SP or Hemokinin 1 (mouse) administrations. The body temperature is maintained constant (36.5±0.5°C) by a thermoregulated heating lamp. About 1?h elapsed between the animal set-up and the start of the experiments, thereafter each animal receive atropine (1.4?μmol/kg i.v. as bolus followed by infusion of 1.4?μM in a volume of 300?μL/h) and 10?min later the vehicle (saline) and increasing doses (0.5 log units) of SP or Hemokinin 1 (mouse) (0.01, 0.03, 0.1, 0.3, 1, 3, 10, 30, and 100?nmol/kg); the first five doses are administered at 20?min intervals, whereas 30?min elapsed between each of the last four doses. Atropine pretreatment is performed in order to minimize the influence of cholinergic secretory reflexes in response to the placement of the cotton swab in the rat's oral cavity for the measurement of salivary secretion induced by SP or Hemokinin 1 (mouse).

参考文献:

[1]. Francesca Bellucci, et al. Pharmacological profile of the novel mammalian tachykinin, hemokinin 1. Br J Pharmacol. 2002 Jan; 135(1): 266-274