Date published: 2026-2-22

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GPR10 Activators

Ligands like cannabidiol, PROGLN and physalaemin directly stimulate GPR10 receptor signaling through orthosteric interactions. Neuropeptides vasopressin and oxytocin activate compensatory mechanisms in GPR10 as a result of coordinated G protein coupling. Other molecules like palmitoylethanolamide and L-DOPA enhance GPR10 expression and functional levels via upstream transcriptional or receptor crosstalk events.

Capsaicin demonstrates how GPR10 modulates the activity of binding partners like TRPV1 channels, and how targeting such proteins can produce indirect GPR10 responses. Allosteric regulators pregnenolone and inverse agonists AM630 and diphenhydramine carefully manipulate GPR10 functionality at receptor complexes or relieve tonic inhibition to optimize downstream signaling.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

AM-630

164178-33-0sc-200365B
sc-200365
sc-200365A
sc-200365C
5 mg
10 mg
50 mg
100 mg
$78.00
$166.00
$634.00
$869.00
8
(1)

AM630 is a CB2 receptor antagonist. GPR10 receptor activity is under tonic inhibition by CB2 receptor signaling in some tissues. By blocking this inhibition, AM630 can relieve repression of GPR10 and indirectly enhance its functional output.

Vasopressin

11000-17-2sc-356188
sc-356188A
5 mg
25 mg
$260.00
$1040.00
1
(0)

Vasopressin engages V1a receptors which couple through Gq proteins. GPR10 couples to Gi/o and cross-talk exists between Gi/o and Gq pathways. Vasopressin activates compensatory mechanisms in GPR10 signaling through this G protein interaction network.

Oxytocin acetate salt

50-56-6sc-279938
sc-279938A
sc-279938B
sc-279938C
sc-279938D
sc-279938E
1 mg
5 mg
25 mg
100 mg
250 mg
1 g
$60.00
$180.00
$337.00
$663.00
$969.00
$1836.00
4
(1)

Similar to vasopressin, oxytocin activates its receptor (also V1a coupled) to indirectly modulate GPR10 activity through coordinated G protein networks. Both neuropeptides precisely enhance GPR10 function through physiology-based activation of these coupled pathways.

Pregnenolone

145-13-1sc-204860
sc-204860A
sc-204860B
sc-204860C
5 g
25 g
100 g
500 g
$87.00
$148.00
$347.00
$1122.00
(1)

Pregnenolone acts as an allosteric modulator of several GPCRs including cannabinoid receptors that regulate GPR10. It fine-tunes GPR10 functional selectivity at receptor complexes to optimize downstream signaling outputs.

Levodopa

59-92-7sc-205372
sc-205372A
5 g
25 g
$54.00
$171.00
9
(1)

L-DOPA enhances dopamine neurotransmission. GPR10 expression is regulated through dopamine D2 receptor coupling and cAMP pathways. L-DOPA treatment activates these mechanisms to augment GPR10 functional levels.

Physalaemin

2507-24-6sc-499389
1 mg
$97.00
(0)

Physalaemin is a compound from frog skin that activates GPR10. It directly stimulates GPR10 to trigger downstream signaling events like calcium mobilization and mitogen activation.

Sarafotoxin 6c

121695-87-2sc-397331
sc-397331A
sc-397331B
sc-397331C
100 µg
500 µg
1 mg
2.5 mg
$423.00
$816.00
$1533.00
$2550.00
1
(0)

Sarafotoxin S6c engages GPR10 as a selective receptor agonist. This results in enhanced GPR10 signaling through canonical receptor:ligand interactions that stimulate intracellular effectors.

Capsaicin

404-86-4sc-3577
sc-3577C
sc-3577D
sc-3577A
50 mg
250 mg
500 mg
1 g
$96.00
$160.00
$240.00
$405.00
26
(1)

Capsaicin activates TRPV1 channels while GPR10 modulates TRPV1 function. Capsaicin treatment stimulates a coordinate response between these coupled systems to indirectly enhance GPR10 activity.

Diphenhydramine hydrochloride

147-24-0sc-204729
sc-204729A
sc-204729B
10 g
25 g
100 g
$52.00
$84.00
$124.00
4
(1)

Diphenhydramine is an H1 receptor inverse agonist. GPR10 signals through H1 receptors and their pathways in some tissues. Diphenhydramine relieves tonic repression of GPR10 by H1 receptors, heightening its functional responsiveness.

Palmitoylethanolamide

544-31-0sc-202754
sc-202754A
sc-202754B
sc-202754C
sc-202754D
10 mg
50 mg
500 mg
1 g
10 g
$80.00
$243.00
$2091.00
$3339.00
$16657.00
(1)

Palmitoylethanolamide activates PPAR-α which regulates GPR10. It boosts GPR10 function through upstream transcriptional control mediated by PPAR-α receptor stimulation.