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Eledoisin (Eledone peptide) Sale

(Synonyms: 依来多辛,Eledone peptide) 目录号 : GC30285

A neurokinin receptor agonist

Eledoisin (Eledone peptide) Chemical Structure

Cas No.:69-25-0

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1mg
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产品描述

Eledoisin is an undecapeptide tachykinin neuropeptide and neurokinin (NK) receptor agonist originally isolated from E. moschata.1,2 It binds to NK1 (pD2 = 9.5 and 9.21 in isolated dog carotid artery and guinea pig ileum, respectively), NK2 (pD2 = 8.22 and 7.7 in isolated rabbit pulmonary artery and rat duodenum, respectively), and NK3 receptors (pD2 = 7.11 and 7.06 in isolated rat portal vein and hamster urinary bladder, respectively).3 Eledoisin induces contraction of isolated guinea pig ileum and rabbit jejunum.4 It also induces salivation in rats and lowers arterial blood pressure in rabbits and guinea pigs in vivo.4,5

1.Severini, C., Improta, G., Falconieri-Erspamer, G., et al.The tachykinin peptide familyPharmacol. Rev.54(2)285-322(2002) 2.Erspamer, V., and Anastasi, A.Structure and pharmacological actions of eledoisin, the active endecapeptide of the posterior salivary glands of EledoneExperientia18(2)58-59(1962) 3.Regoli, D., Drapeau, G., Dion, S., et al.Receptors for substance P and related neurokininsPharmacology38(1)1-15(1989) 4.Holzer-Petsche, U., Schimek, E., Amann, R., et al.In vivo and in vitro actions of mammalian tachykininsNaunyn Schmiedebergs Arch. Pharmacol.330(2)130-135(1985) 5.Hancock, J.C., and Hoover, D.B.Effect of substance P and other tachykinins on arterial pressure in guinea-pigsJ. Auton. Pharmacol.5(1)25-30(1985)

Chemical Properties

Cas No. 69-25-0 SDF
别名 依来多辛,Eledone peptide
Canonical SMILES {Glp}-Pro-Ser-Lys-Asp-Ala-Phe-Ile-Gly-Leu-Met-NH2
分子式 C54H85N13O15S 分子量 1188.4
溶解度 Water : 18.15 mg/mL (15.27 mM) 储存条件 Store at -20°C
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1 mM 0.8415 mL 4.2073 mL 8.4147 mL
5 mM 0.1683 mL 0.8415 mL 1.6829 mL
10 mM 0.0841 mL 0.4207 mL 0.8415 mL
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Research Update

Occurrence and some properties of eledoisin in extracts of posterior salivary glands of Eledone

The posterior salivary glands of Eledone, alone among the tissues of this molluscan species, contain eledoisin, an endecapeptide with activity on blood vessels and extravascular smooth muscles. The salivary glands of Octopus vulgaris and O. macropus lack the polypeptide. Eledoisin is present, in amounts ranging from 20 to 160 mug/g fresh tissue, at all stages of growth and in every season; however, conspicuous differences in the eledoisin content were observed in different groups of animals. Eledoisin is fairly stable in intact salivary glands stored on ice. The most suitable solvent for its extraction is 70 to 80% methanol. Better results are also obtained with boiling diluted acetic acid, than with ethanol, whereas extraction with acetone gives unsatisfactory yields. Eledoisin is stable in neutral or slightly acid medium, but is rapidly destroyed by strong acids and even more rapidly by strong alkalis. It is quickly and completely inactivated by chymotrypsin, and somewhat more slowly and incompletely by trypsin. Carboxypeptidase is ineffective. Passage of crude salivary extracts of Eledone through an alumina column yields preparations of eledoisin which may be considered pure from a biological point of view.

Structure and pharmacological actions of eledoisin, the active endecapeptide of the posterior salivary glands of Eledone

The isolation and amino acid sequence of eledoisin, the active endecapeptide of the posterior salivary glands of Eledone

[Special indications for the use of soft contact lenses as a drug-release-system (author's transl)]

Research has been performed, both experimentally and clinically, to establish the value of the association of soft contact lenses and some types of eye drops. The use of soft contact lenses with eye drops may be useful in some special cases: a) more prolonged and more sustained effect compared with the usual way of administration of eye drops (especially antiglaucomatous substances, antimetabolites, mydriatics); b) possibility of reducing the concentration to avoid local discomfort or systemic side-effects, without loss of their effectiveness on the eye conditions to be treated. The combined use of soft lenses (12.5-15 mm in diameter) with eye drops may be obtained either by presoaking the lens in the liquid or by regular instillation of eye drops after insertion of the lens; the two techniques may of course be associated. In the present research the advantages of utilizing hydrophylic lenses with osmotically active substances, to obtain a better and more protracted dehydration of the cornea, were first examined, in vitro and in vivo. The following substances were tested: 10% propylenglycol, 10% glycerol, 10% glucose and 5% natrium chloride. The clearing effect of the different types of treatment was evaluated in 45 patients with edematous bullous keratopathy with an instrument which measured the infrared light emitted by an optic fiber and reflected by the cornea. The effects were more marked for the epithelial than for the stromal oedema. Another group of investigations was performed with two polypeptides with high molecular weight: Eledoisin, extracted from a mediterranean octopus, Eledone moschata, and Physalaemin, extracted from the skin of a south american batrachian, Physalaemus fuscomaculatus, both of these stimulate the lacrimal secretion and were previously successfully employed topically by the authors against keratoconjunctivitis sicca. The increase of the amount of fluid was however short-lived. Eledoisin at a concentration of 200 mug/ml, was examined in its effects both in vitro and in vivo, whereas physalaemin, at a concentration of 20 mug/ml, only in vitro, owing to the present shortage of the product. The clinical tests in 23 eyes of 14 patients with keratoconjunctivitis sicca proved satisfactory, since the lacrymal stimulating effect is not only greater, but lasts three times longer by combining the instillation of eledoisin with a presoaked soft lens. Some antiglaucomatous products (propranolol, clonidine, prostigmine) were, finally, used in association with a soft lens to reduce the concentration of the eye drops for a better tolerance locally (propranolol: a beta-adrenergic blocking agent) or generally (clonidine: alpha-adrenergic agent), also with the advantage of protracted release. With propranolol the concentration could be reduced to 0.01-0,10% (instead of 0.125 to 0.25%) and to 1.5% (instead of 3%) with prostigmine, when lenses were presoaked or instillations took place at regular time intervals, after insertion of the lenses.

[Effects of eledoisin on water intake induced by subcutaneous injection of hypertonic NaCl in the rat]

Intracerebroventricular administration of eledoisin, the tachykinin peptide of the salivary glands of Eledone Moschata, exerts a potent and long-lasting inhibition of water intake induced by the subcutaneous administration of hypertonic NaCl in the rat. The inhibitory effect is statistically significant up to 6 hr following eledoisin treatment, while the 24 hr water intake in control and treated rats is essentially identical. The results of the present study demonstrate that the long-lasting effect is not due to increased renal excretion of the osmotic load, nor, likely, to larger production of metabolic water. Probably, eledoisin exerts an inhibitory effect of such a long duration by means of central actions which last well beyond its half-life, or, alternatively, by promoting an increased excretion of the osmotic load through elimination routes different from the kidney.