Date published: 2025-11-23

1-800-457-3801

SCBT Portrait Logo
Seach Input

NK-1R Activators

The neurokinin-1 receptor (NK-1R) is a member of the tachykinin family of G-protein coupled receptors. The tachykinins are a group of peptides that play a significant role in various physiological functions, such as the transmission of nerve impulses, modulation of pain, and regulation of various cellular functions. NK-1R, specifically, is predominantly involved in the binding and activity of substance P, a prominent member of the tachykinin family. Activators of NK-1R, as the name suggests, are molecules or compounds that stimulate or enhance the activity of this receptor, leading to a heightened response to its natural ligand or inducing a similar response even in the absence of the ligand. The mechanism of action of NK-1R activators can vary. Some might directly bind to the receptor, mimicking the natural ligand's action, thereby inducing the intracellular cascade of events typical of NK-1R activation. Others might work allosterically, binding to sites on the receptor other than the primary ligand-binding site, which either enhances the affinity of the receptor for its ligand or modulates its activity to elicit a response. The diverse nature of these activators can be attributed to the variety of molecular structures and sizes they encompass, from small molecules to larger peptides. These activators are crucial for understanding the intrinsic functionalities and intricacies of the NK-1R, shedding light on its pivotal roles in the realm of cellular signaling and overall physiological homeostasis.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Substance P

sc-3137
1 mg
$95.00
(0)

Substance P acts as a neuropeptide that selectively binds to the neurokinin-1 receptor (NK-1R), facilitating intricate signaling pathways. Its unique structure allows for specific conformational changes upon receptor binding, triggering downstream effects in cellular communication. The peptide's interactions are characterized by a high affinity for NK-1R, leading to rapid receptor activation and subsequent modulation of intracellular signaling cascades, influencing various physiological responses.

Neurokinin A

sc-3138
1 mg
$95.00
(0)

Neurokinin A is a neuropeptide that engages with the neurokinin-2 receptor (NK-2R), initiating a cascade of intracellular signaling events. Its distinct amino acid sequence enables it to form stable complexes with the receptor, promoting conformational shifts that enhance receptor activation. This interaction influences calcium ion influx and phospholipase C activity, leading to the generation of second messengers that modulate diverse cellular functions and responses.

Substance P

33507-63-0sc-201169
1 mg
$55.00
(1)

Substance P is a neuropeptide that selectively binds to the neurokinin-1 receptor (NK-1R), triggering a series of intracellular signaling pathways. Its unique structure allows for high-affinity interactions, facilitating receptor dimerization and subsequent activation. This engagement leads to the activation of protein kinase C and the release of intracellular calcium, which play critical roles in modulating synaptic transmission and neuronal excitability. The kinetics of this interaction are characterized by rapid binding and a sustained signaling response, highlighting its role in neurogenic inflammation and pain pathways.

[Sar-9, Met(O2)-11]-Substance P

110880-55-2sc-201170
1 mg
$127.00
(0)

[Sar-9, Met(O2)-11]-Substance P is a modified neuropeptide that exhibits enhanced binding affinity for the neurokinin-1 receptor (NK-1R). Its structural modifications promote unique conformational dynamics, allowing for distinct receptor interactions that influence downstream signaling cascades. This compound demonstrates altered reaction kinetics, with a pronounced effect on G-protein coupling efficiency, leading to varied intracellular responses. The peptide's stability and resistance to enzymatic degradation further enhance its functional profile, making it a subject of interest in receptor biology.

[Pro9] Substance P

104486-69-3sc-396074
sc-396074A
500 µg
2.5 mg
$75.00
$188.00
(0)

Pro9 Substance P is a neuropeptide analog characterized by its high specificity for the neurokinin-1 receptor (NK-1R). Its unique amino acid substitutions facilitate selective receptor activation, triggering specific intracellular signaling pathways. The compound exhibits distinct molecular interactions that enhance receptor dimerization and modulate downstream effects. Additionally, its structural resilience contributes to prolonged bioactivity, making it a compelling subject for studies on receptor-mediated signaling mechanisms.