1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. trans-ACPD

trans-ACPD (Synonyms: Trans-(±)-ACP)

Cat. No.: HY-19434 Purity: >98.0%
Handling Instructions

trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.

For research use only. We do not sell to patients.

trans-ACPD Chemical Structure

trans-ACPD Chemical Structure

CAS No. : 67684-64-4

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10 mM * 1 mL in DMSO USD 79 In-stock
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2 mg USD 72 In-stock
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5 mg USD 108 In-stock
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10 mg USD 180 In-stock
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25 mg USD 360 In-stock
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50 mg USD 660 In-stock
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100 mg USD 1188 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.

IC50 & Target[1]

mGluR

 

In Vitro

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].

In Vivo

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].

Molecular Weight

173.17

Formula

C₇H₁₁NO₄

CAS No.

67684-64-4

SMILES

O=C([[email protected]]1(N)C[[email protected]@H](C(O)=O)CC1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (288.73 mM; Need ultrasonic)

H2O : 3.57 mg/mL (20.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (14.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (14.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[3]

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.).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

trans-ACPDTrans-(±)-ACPmGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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