Sigma Receptor Agonist

Sigma Receptor Agonists (31):

Cat. No.	Product Name	Effect	Purity

HY-18100A

PRE-084 hydrochloride	Agonist	99.79%
PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

HY-13510

Cutamesine dihydrochloride	Agonist	98.01%
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes.

HY-116586

AF710B	Agonist
AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.

HY-111081C

(±)-PPCC oxalate	Agonist
(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with K_i of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.

HY-101864

Blarcamesine hydrochloride	Agonist	99.87%
Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC₅₀ of 860 nM.

HY-B2215

Dimemorfan phosphate	Agonist	99.87%
Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.

HY-14221A

Siramesine hydrochloride	Agonist	99.74%
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.

HY-134004

Pentoxyverine	Agonist	98.91%
Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

HY-B1055

Pentoxyverine citrate	Agonist	99.63%
Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with K_is of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.

HY-14218

Ditolylguanidine	Agonist	99.03%
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with K_i values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer.

HY-B1216

Oxeladin citrate	Agonist	≥98.0%
Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (K_i = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research.

HY-100155

4-IBP	Agonist	99.81%
4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).

HY-149804

S1R agonist 2	Agonist	≥98.0%
S1R agonist 2 (Compound 8b) is a selective S1R agonist with K_is of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

HY-116594

OPC-14523 free base	Agonist
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC₅₀=47/56 nM), the 5-HT1A receptor (IC₅₀=2.3 nM), and the 5-HT transporter (IC₅₀=80 nM). OPC-14523 free base shows antidepressant-like activity.

HY-116463

E1R	Agonist	99.28%
E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.

HY-14813

Cutamesine	Agonist
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.

HY-105296

Blarcamesine	Agonist	99.51%
Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.

HY-14221B

Siramesine fumarate	Agonist
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.

HY-149803

S1R agonist 1	Agonist	≥98.0%
S1R agonist 1 (Compound 6b) is a selective S1R agonist with K_is of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

HY-149803A

S1R agonist 1 hydrochloride	Agonist	99.83%
S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with K_is of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

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