α,β-Methylene-ATP 

α,β-Methylene-ATP is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system^[1][2][3].

Electrophysiological activity: α,β-Methylene-ATP (10 μM; 3 seconds) evokes a fast inward current in rat dorsal root ganglion (DRG) neurons, associated with P2X3 receptor activation. 10 μM Diinosine pentaphosphate (Ip5I) can significantly inhibit this inward current^[1].
α,β-Methylene-ATP (10 μM; transient) enhances the amplitude of the current evoked by Acetylcholine (HY-B0282) in rat adrenal medullary chromaffin cells and increases the proportion of the current sensitive to α-conotoxin RgIA (HY-P5845)^[1].

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

α,β-Methylene-ATP (5-50 μg/kg; left popliteal artery injection; single dose) induces a reflex pressor response in the decerebrate cat model, which is blocked by sciatic nerve transection or the P2X receptor antagonist PPADS (HY-108960) (10 mg/kg; left popliteal artery injection)^[2].
α,β-Methylene-ATP (10 nmol/rat; intracerebroventricular injection; single dose) produces an anti-mechanical nociceptive effect in Sprague-Dawley rats, which is significantly attenuated by pretreatment with DSP-4 (HY-121602/HY-103210) (10 mg/kg DSP-4; intraperitoneal injection)^[3].
α,β-Methylene-ATP (0.1-1 nmol/side; bilateral microinjection into the locus coeruleus; single dose) increases the pain threshold of Sprague-Dawley rats in a dose-dependent manner, an effect that could be antagonized by co-injection of PPADS (HY-108960) (0.1-1 nmol/side)[3].

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

505.21

C₁₁H₁₈N₅O₁₂P₃

7292-42-4

OP(OP(CP(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C3=NC=NC(N)=C3N=C2)O1)(O)=O)(O)=O)(O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Arribas-Blázquez M, et al. Overexpression of P2X3 and P2X7 Receptors and TRPV1 Channels in Adrenomedullary Chromaffin Cells in a Rat Model of Neuropathic Pain. Int J Mol Sci. 2019 Jan 3;20(1).  [Content Brief]

  [2]. Hanna RL, et al. alpha,beta-Methylene ATP elicits a reflex pressor response arising from muscle in decerebrate cats. J Appl Physiol (1985). 2002 Sep;93(3):834-41.  [Content Brief]

  [3]. Fukui M, et al. Involvement of locus coeruleus noradrenergic neurons in supraspinal antinociception by alpha,beta-methylene-ATP in rats. J Pharmacol Sci. 2004 Feb;94(2):153-60  [Content Brief]