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Merck

A6478

Sigma-Aldrich

(R,S)-AM1241

≥98% (HPLC), solid

别名:

(R,S)-3-(2-Iodo-5-nitrobenzoyl)-1-(1-methyl-2-piperidinylmethyl)-1H-indole

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About This Item

经验公式(希尔记法):
C22H22IN3O3
分子量:
503.33
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

solid

藥物控制

regulated under CDSA - not available from Sigma-Aldrich Canada

顏色

yellow

溶解度

DMSO: ~18 mg/mL at 60 °C

SMILES 字串

CN1CCCCC1Cn2cc(C(=O)c3cc(ccc3I)[N+]([O-])=O)c4ccccc24

InChI

1S/C22H22IN3O3/c1-24-11-5-4-6-16(24)13-25-14-19(17-7-2-3-8-21(17)25)22(27)18-12-15(26(28)29)9-10-20(18)23/h2-3,7-10,12,14,16H,4-6,11,13H2,1H3

InChI 密鑰

ZUHIXXCLLBMBDW-UHFFFAOYSA-N

應用

(R,S)-AM1241 has been used as a cannabinoid CB2 agonist:
  • to study its inhibitory effect on bone cancer-induced pain and bone loss
  • to study the effect of its interaction with 17βestradiol on proliferation activity in primary human osteoblasts
  • to evaluate the sites of CB2 mediated antinociception in vivo.

生化/生理作用

AM1241 acts as an antinociceptive agent in several animal pain models. It has a potential to delay disease progression in amyotrophic lateral sclerosis (ALS) mouse model. Intrathecal, intravenous or intraperitoneal administration of AM1241 reduces hyperalgesia and allodynia in neuropathic rats.
Selective CB2 cannabinoid receptor agonist

象形圖

Health hazardExclamation mark

訊號詞

Danger

危險分類

Eye Irrit. 2 - Resp. Sens. 1 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Faceshields, Gloves


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Elizabeth J Rahn et al.
Pharmacology, biochemistry, and behavior, 98(4), 493-502 (2011-03-09)
Cannabinoid CB(2) agonists produce antinociception without central nervous system (CNS) side-effects. This study was designed to characterize the pharmacological and antinociceptive profile of AM1710, a CB(2) agonist from the cannabilactone class of cannabinoids. AM1710 did not exhibit off-target activity at
A G Nackley et al.
Neuroscience, 119(3), 747-757 (2003-06-18)
Activation of cannabinoid CB(2) receptors attenuates thermal nociception in untreated animals while failing to produce centrally mediated effects such as hypothermia and catalepsy [Pain 93 (2001) 239]. The present study was conducted to test the hypothesis that activation of CB(2)
AM1241, a cannabinoid CB2 receptor selective compound, delays disease progression in a mouse model of amyotrophic lateral sclerosis
Kim K, et al.
European Journal of Pharmacology, 542(1-3), 100-105 (2006)
The cannabinoid CB2 receptor-specific agonist AM1241 increases pentylenetetrazole-induced seizure severity in Wistar rats
de Carvalho CR, et al.
Epilepsy Research, 127(2), 160-167 (2016)
A synergistic interaction of 17-$\beta$-estradiol with specific cannabinoid receptor type 2 antagonist/inverse agonist on proliferation activity in primary human osteoblasts
Hojnik M, et al.
Biomedical Reports, 3(4), 554-558 (2015)

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