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Galantide Sale

(Synonyms: 多克隆抗体) 目录号 : GC30931

Galantide是一种可逆的非特异性甘丙肽受体拮抗剂。

Galantide Chemical Structure

Cas No.:138579-66-5

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500μg
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1mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Rats: Galantide is dissolved in 0.9% NaCl. The i.c.v. injection is given to the resident rat immediately after removal of the juvenile, at the end of the first encounter. Control rats receive an equal volume (4 µL) of saline by the same route, at the same infusion rate (1 µL/20 s) and at the same time. A minimum of 10 adult rats are used for each dose level[4]. Mice: Galantide stock solution is prepared in 0.01% bovine serum albumin in saline. The mice are allocated to 7 groups: Mice administered the vehicle for injection (saline alone), mice administered only caerulein (AP alone), mice administered only galantide (GT alone) or feG (feG alone), mice administered caerulein and galantide (AP+GT) or caerulein and feG (AP+feG) and finally mice that are administered with caerulein, galantide and feG (AP+GT+feG). On the day prior to the AP induction, a blood sample is collected to measure the basal plasma amylase activity[3].

References:

[1]. Lindskog S, et al. The novel high-affinity antagonist, galantide, blocks the galanin-mediatedinhibition of glucose-induced insulin secretion. Eur J Pharmacol. 1992 Jan 14;210(2):183-8.
[2]. Benelli A, et al. Galantide stimulates sexual behaviour in male rats. Eur J Pharmacol. 1994 Aug 1;260(2-3):279-82.
[3]. Barreto SG, et al. The efficacy of combining feG and galantide in mild caerulein-induced acutepancreatitis in mice. Peptides. 2010 Jun;31(6):1076-82.
[4]. Arletti R, et al. Galantide improves social memory in rats. Pharmacol Res. 1997 Apr;35(4):317-9.

产品描述

Galantide is a reversible and non-specific galanin receptor antagonist.

Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. The antagonist is also found to displace 125I-monoiodo-[TyrZ6]galanin from membranes of the insulin producing Rin m 5F cells with an IC50 value of less than 0.1 nM[1].

Intracerebroventricular injection of galanin (5 micrograms/rat) inhibited sexual behavior in experienced male rats--without producing any other locomotor or behavioral deficit-, injection of the galanin antagonist, galantide, by the same route (1 or 2 micrograms/rat) stimulated sexual behavior (improving arousal, motivation and performance indexes) and antagonized the effect of galanin[2]. Galantide ameliorates mild acute pancreatitis (AP). Galantide significantly reduces AP-induced hyperenzymemia by 41-49%[3]. Galantide has been found to improve social memory in 'socialrecognition' test when i.c.v. administered at doses varying from 6-6000 nM[4].

[1]. Lindskog S, et al. The novel high-affinity antagonist, galantide, blocks the galanin-mediatedinhibition of glucose-induced insulin secretion. Eur J Pharmacol. 1992 Jan 14;210(2):183-8. [2]. Benelli A, et al. Galantide stimulates sexual behaviour in male rats. Eur J Pharmacol. 1994 Aug 1;260(2-3):279-82. [3]. Barreto SG, et al. The efficacy of combining feG and galantide in mild caerulein-induced acutepancreatitis in mice. Peptides. 2010 Jun;31(6):1076-82. [4]. Arletti R, et al. Galantide improves social memory in rats. Pharmacol Res. 1997 Apr;35(4):317-9.

Chemical Properties

Cas No. 138579-66-5 SDF
别名 多克隆抗体
Canonical SMILES Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2
分子式 C104H151N25O26S 分子量 2199.53
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mM 0.4546 mL 2.2732 mL 4.5464 mL
5 mM 0.0909 mL 0.4546 mL 0.9093 mL
10 mM 0.0455 mL 0.2273 mL 0.4546 mL
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Research Update

Octreotide negates the benefit of galantide when used in the treatment of caerulein-induced acute pancreatitis in mice

Background: We have previously shown that galantide, a non-specific galanin receptor antagonist, ameliorates acute pancreatitis (AP) induced in mice. Octreotide, a somatostatin analogue, has been used in the treatment of AP with inconsistent outcomes. This study set out to compare the efficacy of a combined treatment of galantide and octreotide with the efficacy of each agent individually in experimental AP. Methods: Acute pancreatitis was induced in mice with 7-hourly caerulein injections. Galantide and/or octreotide were co-administered with each caerulein injection commencing with the first injection. Control animals received galantide, octreotide or saline alone. Pancreata were harvested for histological examination and estimation of myeloperoxidase (MPO) activity. Plasma amylase and lipase activities were measured. Results: Galantide significantly reduced AP-induced hyperenzymaemia by 39-45%. Octreotide alone, or in combination with galantide, did not significantly alter AP-induced hyperenzymaemia. Plasma enzyme activity in the control groups was comparable with pre-treatment activity. Galantide and octreotide administered individually reduced MPO activity by 79% and 50%, respectively; however their combination was without effect. Galantide, octreotide and their combination significantly reduced the percentage of abnormal acinar cells by 28-45%. Conclusions: Treatment with galantide alone ameliorated most of the indices of AP studied, whereas treatment with octreotide reduced pancreatic MPO activity and acinar cell damage. Combining the two peptides appears to negate their individual benefits, which suggests an interaction in their mechanism of action.

Galantide improves social memory in rats

The role of galanin in memory paradigms has been largely evaluated. The galanin-antagonist galantide, a chimeric peptide obtained from amino acids 1-13 of galanin attached to the C-terminal fragment of bradykinin, has been found to improve social memory in 'social recognition' test when i.c.v. administered at doses varying from 6-6000 nmoles.

The efficacy of combining feG and galantide in mild caerulein-induced acute pancreatitis in mice

We have previously shown that galantide ameliorates mild acute pancreatitis (AP), and the salivary tripeptide analogue, feG, ameliorates severe AP in mice. In this study, we compared the efficacy of combining galantide and feG with that of the individual agents in treating mild AP induced in mice with 7-hourly caerulein injections. Galantide was co-administered with each caerulein injection commencing with the first injection. feG was co-administered with the first injection of caerulein as a single intraperitoneal injection. Combination of the agents was also administered. Control animals received galantide, feG, or saline alone. Pancreata were harvested for histological examination and estimation of myeloperoxidase (MPO) activity. Plasma enzyme activities were measured. Galantide significantly reduced AP-induced hyperenzymemia by 41-49%. The combination of galantide and feG significantly reduced AP-induced hyperenzymemia by 39-40%, whereas feG alone was without effect. Plasma enzyme activity in the control groups was comparable with pre-treatment activity. Galantide, feG, and their combination significantly reduced MPO activity by 83, 44 and 74% respectively, and % abnormal acinar cells by 32, 29 and 36% respectively. This study demonstrates for the first time the beneficial effect of feG in mild caerulein-induced AP. Moreover the data indicate that the hyperenzymemia in mild caerulein-induced AP at 12h possibly reflect a larger secretory component as compared to enzyme release due to neutrophil-mediated acinar cell damage. The effects of the treatment with both peptides indicate a possible role for galantide in modulating neutrophil chemotaxis/activation and supports the hypothesis that galantide may influence neurogenic inflammation in AP.

Galantide stimulates sexual behaviour in male rats

While intracerebroventricular injection of galanin (5 micrograms/rat) inhibited sexual behavior in experienced male rats--without producing any other locomotor or behavioral deficit-, injection of the galanin antagonist, galantide, by the same route (1 or 2 micrograms/rat) stimulated sexual behavior (improving arousal, motivation and performance indexes) and antagonized the effect of galanin. These data further suggest that galanin plays a physiological role in male sexual behavior.

Nitric oxide-mediated erectile effects of galantide but not galanin in vivo

The purpose of this study was to investigate the in vivo effects of intracavernosal injections of galanin and galantide (a specific galanin receptor antagonist) on penile erection in the anesthetized cat. Erectile responses to galanin and galantide were compared with responses to a standard triple drug combination [1.65 mg papaverine, 25 microg phentolamine, and 0.5 microg prostaglandin E(1) (PGE(1))]. Intracavernosal injections of galanin (3-100 nmol) and galantide (0. 1-3 nmol) induced penile erection in a dose-dependent manner. In terms of relative potency, galantide was approximately 100-fold more potent than galanin at increasing cavernosal pressure. The maximal increases in intracavernosal pressure in response to galanin and galantide were 83 and 95%, respectively, of the control triple drug combination. The total durations of erectile response caused by these peptides were significantly shorter (P<0.05) than those by the triple drug combination. The nitric oxide synthase inhibitor L-NAME (20 mg) significantly decreased the erectile response in the cat to galantide but not to galanin, while the K(+)(ATP) channel antagonist U-37883A (3 mg) had no effect on the erectile response to galanin nor galantide. The results of the present study demonstrate that galantide, a putative antagonist for the galanin receptor, has more potent agonist activity than galanin in increasing intracavernosal pressure in the cat. Moreover, these data suggest that galantide, but not galanin, causes penile erection by an NO/cGMP-dependent mechanism. This is the first study to demonstrate that galanin may play a role in the physiology of penile erection.