SA4503

Modify Date: 2024-01-02 11:19:54

SA4503 Structure
SA4503 structure
Common Name SA4503
CAS Number 165377-43-5 Molecular Weight 368.51200
Density N/A Boiling Point N/A
Molecular Formula C23H32N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SA4503


SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.IC50 value: 17.4 nM [1]Target: σ1R agonistin vitro: SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain [1]. At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner [3].in vivo: The intravenous administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter the firing rate or pattern of spontaneously active DA neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of SA4503 did not alter the number of spontaneously active SNC and VTA DA neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503 produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively[2]. SA4503 suppressed the progression of ALS in an SOD1(G93A) ALS mouse model. SA4503 did not affect the onset time of ALS. However, it significantly extended the survival time in the SOD1(G93A) mice compared with a vehicle-treated group [3].

 Names

Name 1-[2-(3,4-Dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine
Synonym More Synonyms

 SA4503 Biological Activity

Description SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.IC50 value: 17.4 nM [1]Target: σ1R agonistin vitro: SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain [1]. At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner [3].in vivo: The intravenous administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter the firing rate or pattern of spontaneously active DA neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of SA4503 did not alter the number of spontaneously active SNC and VTA DA neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503 produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively[2]. SA4503 suppressed the progression of ALS in an SOD1(G93A) ALS mouse model. SA4503 did not affect the onset time of ALS. However, it significantly extended the survival time in the SOD1(G93A) mice compared with a vehicle-treated group [3].
Related Catalog
References

[1]. Matsuno K, et al. Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol. 1996 Jun 13;306(1-3):271-9.

[2]. Minabe Y, et al. Acute and chronic administration of the selective sigma1 receptor agonist SA4503 significantly alters the activity of midbrain dopamine neurons in rats: An in vivo electrophysiological study. Synapse. 1999 Aug;33(2):129-40.

[3]. Ono Y, et al. SA4503, a sigma-1 receptor agonist, suppresses motor neuron damage in in vitro and in vivo amyotrophic lateral sclerosis models. Neurosci Lett. 2014 Jan 24;559:174-8.

 Chemical & Physical Properties

Molecular Formula C23H32N2O2
Molecular Weight 368.51200
Exact Mass 368.24600
PSA 24.94000
LogP 3.37250
Storage condition 2-8℃

 Synthetic Route

~86%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Li, Yan; Wang, Xia; Zhang, Jinming; Deuther-Conrad, Winnie; Xie, Fang; Zhang, Xiaojun; Liu, Jian; Qiao, Jinping; Cui, Mengchao; Steinbach, Joerg; Brust, Peter; Liu, Boli; Jia, Hongmei Journal of Medicinal Chemistry, 2013 , vol. 56, # 9 p. 3478 - 3491

~%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Fujimura, Ken-Ichi; Matsumoto, Junzo; Niwa, Masashi; Kobayashi, Tadayuki; Kawashima, Yoichi; In, Yasuko; Ishida, Toshimasa Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1675 - 1683

~%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Fujimura, Ken-Ichi; Matsumoto, Junzo; Niwa, Masashi; Kobayashi, Tadayuki; Kawashima, Yoichi; In, Yasuko; Ishida, Toshimasa Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1675 - 1683

~%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Fujimura, Ken-Ichi; Matsumoto, Junzo; Niwa, Masashi; Kobayashi, Tadayuki; Kawashima, Yoichi; In, Yasuko; Ishida, Toshimasa Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1675 - 1683

~%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Fujimura, Ken-Ichi; Matsumoto, Junzo; Niwa, Masashi; Kobayashi, Tadayuki; Kawashima, Yoichi; In, Yasuko; Ishida, Toshimasa Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 8 p. 1675 - 1683

~%

SA4503 Structure

SA4503

CAS#:165377-43-5

Literature: Li, Yan; Wang, Xia; Zhang, Jinming; Deuther-Conrad, Winnie; Xie, Fang; Zhang, Xiaojun; Liu, Jian; Qiao, Jinping; Cui, Mengchao; Steinbach, Joerg; Brust, Peter; Liu, Boli; Jia, Hongmei Journal of Medicinal Chemistry, 2013 , vol. 56, # 9 p. 3478 - 3491

 Synonyms

Cutamesine
UNII-9J7A4144BX
SA4503