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M40 Sale

目录号 : GC13801

M40,一种多肽性甘丙肽拮抗剂,是一种29个氨基酸的神经肽,广泛分布于大鼠和人的中枢神经系统。

M40 Chemical Structure

Cas No.:143896-17-7

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1mg
¥1,638.00
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Sample solution is provided at 25 µL, 10mM.

Description

M40, a peptidergic galanin antagonist, is a 29 amino acid neuropeptide that is widely distributed in the central nervous system of both rats and humans[1]. M40 significantly blocked galanin-induced feeding in satiated rats[2]. M40, is high-affinity ligands at the spinal cord galanin receptors characterized with Kd values of 6.8±2.2nM[3].

M40 (10μM; 3h) increased insulin release from RIN5AH cells in the absence of galanin[4]. M40 (100nM; 5min) significantly reversed the galanin (100nM; 5min) induced inhibition effect in nucleus tractus solitarius (NTS) neurons[5].

M40 (1.0nmol; 50 min; intracisternal injection) can produce a significant increase on mean arterial pressure of rat[6]. M40 (0.02-2.0nmol; bilateral microinjections; 15min) in lateral septum (LS) dose dependently reduced defensive burying behavior in rats[7].

References:
[1] MCDONALD M P, CRAWLEY J N. Galanin receptor antagonist M40 blocks galanin-induced choice accuracy deficits on a delayed-nonmatching-to-position task [J]. Behavioral neuroscience, 1996, 110(5): 1025-32.
[2] CRAWLEY J N, ROBINSON J K, LANGEL U, et al. Galanin receptor antagonists M40 and C7 block galanin-induced feeding [J]. Brain research, 1993, 600(2): 268-72.
[3] XU X J, WIESENFELD-HALLIN Z, LANGEL U, et al. New high affinity peptide antagonists to the spinal galanin receptor [J]. Br J Pharmacol, 1995, 116(3): 2076-80.
[4] WANG Z L, KULKARNI R N, WANG R M, et al. Possible evidence for endogenous production of a novel galanin-like peptide [J]. J Clin Invest, 1997, 100(1): 189-96.
[5] YUAN C S, DEY L, XIE J T, et al. Gastric effects of galanin and its interaction with leptin on brainstem neuronal activity [J]. The Journal of pharmacology and experimental therapeutics, 2002, 301(2): 488-93.
[6] KHOSHBOUEI H, CECCHI M, DOVE S, et al. Behavioral reactivity to stress: amplification of stress-induced noradrenergic activation elicits a galanin-mediated anxiolytic effect in central amygdala [J]. Pharmacol Biochem Behav, 2002, 71(3): 407-17.
[7] ECHEVARRIA D J, HERNANDEZ A, DIOGENES A, et al. Administration of the galanin antagonist M40 into lateral septum attenuates shock probe defensive burying behavior in rats [J]. Neuropeptides, 2005, 39(5): 445-51.

M40,一种多肽性甘丙肽拮抗剂,是一种29个氨基酸的神经肽,广泛分布于大鼠和人的中枢神经系统[1]。M40显著抑制了饱腹大鼠中甘丙肽诱导的进食行为[2]。M40是脊髓丙氨酸受体的高亲和力配体,Kd值为6.8±2.2nM[3]

M40(10μM; 3h)在不含丙氨酸的情况下增加了RIN5AH细胞的胰岛素释放[4]。M40(100nM; 5min)显著逆转了丙氨酸(100nM; 5min)诱导的NTS(nucleus tractus solitarius,孤束核)神经元抑制作用[5]

使用M40(1.0nmol; 50 min; intracisternal injection)处理大鼠,M40使大鼠平均动脉压显著升高[6]。使用M40(0.02-2.0nmol; bilateral microinjections into LS; 15min)双侧显微注射处理大鼠LS(lateral septum,大脑侧隔),M40剂量依赖性地降低了大鼠的防御性埋地行为[7]

实验参考方法

Cell experiment [1]:

Cell lines

Nucleus tractus solitarius (NTS) neurons

Preparation Method

After the Sprague-Dawley neonatal rats was deeply anesthetized with halothane, a craniotomy was performed, and the forebrain was ablated at the caudal border of the pons by transection. The caudal brainstem and cervical spinal cord were isolated by dissection inmodified Krebs’ solution that contained 128.0mM NaCl, 3.0mM KCl, 0.5mM NaH2PO4, 1.5mM CaCl2, 1.0mM MgSO4, 21mM NaHCO3, 1.0mM mannitol, 30.0mM glucose, and 10.0mM HEPES.

The stomach, connected to the esophagus with the vagus nerves linking it to the brainstem, was kept, and all the other internal organs were removed. The preparation was then isolated and pinned, with the dorsal surface up, on a layer of Sylgard resin in a recording chamber. An incision was made on the lateral surface of the stomach wall to minimize possible gastric vagal fiber damage. The stomach was opened, and its contents were removed. The stomach was then pinned down, and both mucosa and serosa were exposed to Krebs’ solution in the gastric compartment. The preparation was superfused with Krebs’ solution at 23±1℃. The bathing solution was aerated continuously with a mixture of 95% O2 and 5% CO2 and adjusted to pH 7.35 to 7.45.

Single tonic unitary discharges were recorded extracellularly in the medial subnucleus of the NTS by glass microelectrodes filled with 3M NaCl, with an impedance of 10 to 20 MΩ . A collision test was applied to identify orthodromic inputs to ensure that only second- or higher-order NTS neurons in the gastric vagal afferent system. Concentrations of galanin and M40 used in the experiment are 100nM. Each test compound was first dissolved in a small volume of Krebs’ solution. The concentrated solution was then applied to the gastric compartment. The final drug concentration in the gastric compartment was calculated based on the amount of concentrated solution and the total Krebs volume in the gastric compartment. Drug solution was applied 5min prior to any pharmacological observation to provide sufficient time for drug delivery to reach a steady-state level. After each observation, drug was washed out from the compartment. The NTS neuronal responses observed during pretrial or pretreatment (control) were compared with post-trial (washout) to confirm that brainstem neuronal activity returned to the control level after washout. .

Reaction Conditions

100nM; 5min

Applications

M40 significantly reversed the galanin induced inhibition effect in nucleus tractus solitarius (NTS) neurons.
Animal experiment [2]:

Animal models

Male specific pathogen-free Sprague-Dawley rats

Preparation Method

The animals were anaesthetized with urethane (1.1g/kg) a and immediately tracheotomized. The femoral artery was cannulated with a plastic catheter containing heparin (50IU/ml, 0.9% NaCl w/v) to record blood pressure and heart rate. and the animal was placed in a stereotaxic frame. The head was flexed 45°, the neck muscles were dissected with an electric knife to avoid bleeding and the atlanto-occipital membrane was exposed. The surgical procedure took 8-10min and the animals were allowed to stabilize for at least 30min. During the whole experiment, the body temperature was maintained at 37.5±0.5℃ by means of a thermostatic blanket.

To study if M40 alone exerts any effect on central 11 cardiovascular parameters, groups of rats: received intracisternal injections of M40 at doses of 1.0nmol.

Dosage form

1.0nmol; 50 min; intracisternal injection

Applications

M40 injected alone produces a significant increase on mean arterial pressure of rat.

References:
[1] YUAN C S, DEY L, XIE J T, et al. Gastric effects of galanin and its interaction with leptin on brainstem neuronal activity [J]. The Journal of pharmacology and experimental therapeutics, 2002, 301(2): 488-93.
[2] NARVáEZ J A, DíAZ-CABIALE Z, HEDLUND P B, et al. The galanin receptor antagonist M40 blocks the central cardiovascular actions of the galanin N-terminal fragment (1-15) [J]. Eur J Pharmacol, 2000, 399(2-3): 197-203.

化学性质

Cas No. 143896-17-7 SDF
化学名 (S,Z)-2-((Z)-((S)-2-((Z)-((2S,3R)-2-((Z)-((S)-2-((Z)-(2-amino-1-hydroxyethylidene)amino)-1-hydroxy-3-(1H-indol-3-yl)propylidene)amino)-1,3-dihydroxybutylidene)amino)-1-hydroxy-4-methylpentylidene)amino)-N'1-((3Z,5S,6Z,8S,9Z,11S,12Z,15Z,17S,18Z,20S)-1-((S)
Canonical SMILES CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/CN)([H])CC1=CNC2=CC=CC=C12)([H])[C@@](O)([H])C)([H])CC(C)C)([H])CC(O)=N)([H])CO)([H])C)([H])CC3=CC=C(O)C=C3)([H])CC(C)C)([H]
分子式 C94H145N23O24 分子量 1981.33
溶解度 Soluble to 1 mg/ml in sterile water 储存条件 Desiccate at -20°C
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1 mM 0.5047 mL 2.5236 mL 5.0471 mL
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