(±)-trans-ACPD (Synonyms: Trans-(±)-ACP) |
رقم الكتالوجGC12394 |
(± ؛) - عبر ACPD ، ناهض مستقبلات التمثيل الغذائي ، ينتج تعبئة الكالسيوم والتيار الداخلي في الخلايا العصبية المخيخية المستزرعة.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 67684-64-4
Sample solution is provided at 25 µL, 10mM.
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
Excitatory amino acid (EAA) analogues activate receptors that are coupled to the increased hydrolysis of phosphoinositides (PIs). In these studies, hippocampal slices are prepared from neonatal rats (6-11 days old) to characterize the effects of EAA analogues on these receptors. The concentrations of trans-ACPD required to evoke half-maximal stimulation (EC50 value) is 51 μM. DL-2-Amino-3-phosphonopropionate (DL-AP3) is also equipotent as an inhibitor of PI hydrolysis stimulated by ibotenate, quisqualate, and trans-ACPD (IC50 values are 480-850 μM)[2].
Intrathecal injection of NMDA, kainate, and trans-ACPD, TNF-α, or IL-1β causes significant (p<0.001) biting behaviour in mice compared to animals injected intrathecally with saline. In all groups, systemic pre-treatment with GM (100 mg/kg, i.p.) significantly (p<0.001) reduces the biting behaviour compared to mice treated with saline (10 mL/kg, i.p.). The greatest effect of GM is observed on the pro-inflammatory cytokines and NMDA, with the following inhibition percentages: TNF-α (92±7%), IL-1β (91±5%), NMDA (69±1%), and trans-ACPD (71±12%). By contrast, at the same dose, GM has no significant effect on the kainate-mediated biting response[3].
Reference:
[1]. Linden DJ, et al. Trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. J Neurophysiol. 1994 May;71(5):1992-8.
[2]. Littman L, et al. Multiple mechanisms for inhibition of excitatory amino acid receptors coupled to phosphoinositide hydrolysis. J Neurochem. 1992 Nov;59(5):1893-904.
[3]. Córdova MM, et al. Polysaccharide glucomannan isolated from Heterodermia obscurata attenuates acute and chronic pain in mice. Carbohydr Polym. 2013 Feb 15;92(2):2058-64.
Animal experiment: | Mice[3]Male Swiss mice (25-35 g) are used. Intrathecal injections are given to fully conscious mice. Briefly, the animals are manually restrained, and a 30-gauge needle connected by a polyethylene tube to a 25 μL Hamilton gas-tight syringe is inserted through the skin and between the vertebrae into the subdural space of the L5-L6 spinal segments. Intrathecal injections (5 μL/site) are administered over a period of 5 s. Biting behaviour is defined as a single head movement directed at the flanks or hind limbs, resulting in contact of the animal's snout with the target organ. The nociceptive response is elicited by NMDA (450 pmol/site, a selective agonist of the NMDA glutamatergic ionotropic receptor), kainate (110 pmol/site, a selective agonist of the kainate subtype of glutamatergic ionotropic receptors), and trans-ACPD (50 nmol/site, a non-selective agonist of metabotropic glutamate receptors, which is active at group I and group II), TNF-α (0.1 pmol/site) and IL-1β (1 pmol/site) or saline (5 μL/site, i.t.). The amount of time the animal spent biting or licking the caudal region is taken as evidence of nociception and is evaluated following local post injections of the following agonists: NMDA (5 min), kainate (4 min), and trans-ACPD TNF-α, and IL-1β (15 min). Animals received GM (100 mg/kg, i.p.) 0.5 h before intrathecal injection of 5 μL of the drugs, while control animals received a similar volume of saline (10 mL/kg, i.p.). |
References: [1]. Linden DJ, et al. Trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. J Neurophysiol. 1994 May;71(5):1992-8. |
Cas No. | 67684-64-4 | SDF | |
المرادفات | Trans-(±)-ACP | ||
Chemical Name | (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid | ||
Canonical SMILES | OC([C@]1(C[C@H](C(O)=O)CC1)N)=O | ||
Formula | C7H11NO4 | M.Wt | 173.17 |
الذوبان | Soluble to 5 mM in sterile water and to 100 mM in 1eq. NaOH | Storage | Store at RT |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 5.7747 mL | 28.8734 mL | 57.7467 mL |
5 mM | 1.1549 mL | 5.7747 mL | 11.5493 mL |
10 mM | 0.5775 mL | 2.8873 mL | 5.7747 mL |
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