Date published: 2026-4-23

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P2X1 Activators

P2X1 Activators play a pivotal role in modulating the activity of the P2X1 receptor, a key protein in rapid synaptic transmission and muscle contraction. Primary among these activators is Adenosine Triphosphate (ATP), the natural agonist for P2X1. ATP binding to P2X1 triggers the opening of the ion channel, facilitating an influx of cations like calcium and sodium, which are crucial for P2X1's physiological functions. Synthetic agonists like α,β-Methylene ATP and 2-Methylthio ATP also bind to P2X1, leading to enhanced receptor activation and cation influx, thereby amplifying P2X1-mediated responses in cellular signaling.In addition to direct agonists, various compounds indirectly influence P2X1 activity through unique mechanisms. Antagonists such as NF449, PPADS, Suramin, Reactive Blue 2, Brilliant Blue G, and TNP-ATP, initially inhibit P2X1 but can lead to a compensatory increase in receptor sensitivity or expression, ultimately enhancing P2X1 activity. This phenomenon of desensitization followed by rebound upregulation ensures the receptor's continued responsiveness and functional integrity. Furthermore, agents like Probenecid, which modulates extracellular ATP levels, indirectly affect P2X1 activation. Zinc and Magnesium play modulatory roles; Zinc influences P2X1 receptor conformation and responsiveness to ATP, while Magnesium competes with calcium at the receptor site, modulating the receptor's activity. Collectively, these P2X1 Activators, through their direct and indirect actions, regulate the functionality of the P2X1 receptor, ensuring its vital role in neurotransmission and muscle contraction is efficiently performed.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

BzATP triethylammonium salt

112898-15-4sc-203862
5 mg
$156.00
4
(1)

BzATP triethylammonium salt is a potent agonist of P2X1 receptors, known for its ability to induce rapid ion channel activation. Its unique triethylammonium moiety enhances solubility and receptor affinity, facilitating swift interactions with the binding site. This compound triggers a pronounced influx of cations, particularly calcium, leading to significant alterations in cellular signaling dynamics. The kinetics of its action are characterized by a quick onset and a brief duration, underscoring its role in modulating purinergic responses.

ATP

56-65-5sc-507511
5 g
$17.00
(0)

ATP directly enhances P2X1 activity by acting as its primary agonist. ATP binding leads to the opening of the P2X1 ion channel, facilitating cation influx, crucial for P2X1's role in neurotransmission and muscle contraction.

NF449

627034-85-9sc-478179
sc-478179A
sc-478179B
10 mg
25 mg
100 mg
$203.00
$469.00
$1509.00
1
(0)

NF449, while known as a P2X1 antagonist, can indirectly enhance P2X1 activity through receptor desensitization followed by a rebound increase in receptor sensitivity or upregulation.

Suramin sodium

129-46-4sc-507209
sc-507209F
sc-507209A
sc-507209B
sc-507209C
sc-507209D
sc-507209E
50 mg
100 mg
250 mg
1 g
10 g
25 g
50 g
$152.00
$214.00
$728.00
$2601.00
$10965.00
$21838.00
$41096.00
5
(1)

Suramin, a P2X1 receptor antagonist, can enhance P2X1 activity indirectly through receptor desensitization and subsequent upregulation or increased receptor responsiveness.

Victoria Blue B

2580-56-5sc-216055
sc-216055A
25 g
100 g
$37.00
$124.00
1
(0)

Reactive Blue 2, known to inhibit P2X1, may indirectly increase P2X1 activity over time by inducing receptor desensitization and compensatory mechanisms leading to receptor upregulation.

Probenecid

57-66-9sc-202773
sc-202773A
sc-202773B
sc-202773C
1 g
5 g
25 g
100 g
$28.00
$39.00
$100.00
$277.00
28
(2)

Probenecid, often used to inhibit organic anion transporters, can indirectly enhance P2X1 activity by modulating extracellular ATP levels, thus potentially influencing P2X1 receptor activation.

Zinc

7440-66-6sc-213177
100 g
$48.00
(0)

Zinc can enhance P2X1 receptor activity by acting as a modulatory agent. It may bind to distinct sites on the receptor, influencing its conformation and responsiveness to ATP.