Hemokinin 1 (mouse, rat) trifluoroacetate salt

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.

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Others

Peptides

Ki: 0.175 nM (Human NK1 receptor), 560 nM (Human NK2 receptor)[1]

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].

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).

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

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