(R,S)-AM1241

Bezeichnung:(R,S)-AM1241

CAS-Nr444912-48-5

Englisch Name:(R,S)-AM1241

CBNumberCB4972473

SummenformelC22H22IN3O3

Molgewicht503.33

MOL-Datei444912-48-5.mol

(R,S)-AM1241 physikalisch-chemischer Eigenschaften

Siedepunkt	630.7±55.0 °C(Predicted)
Dichte	1.60±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	DMSO: ~18mg/mL at 60°C
pka	9.73±0.10(Predicted)
Aggregatzustand	solid
Farbe	yellow

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	36/37/38-42/43
S-Sätze:	22-26-36/37-45
WGK Germany	3

Gefahreninformationscode (GHS)

(R,S)-AM1241 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R42/43:Sensibilisierung durch Einatmen und Hautkontakt möglich.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
AM1241 is a cannabinoid (CB) receptor agonist that is selective for CB₂ over CB₁ with K_i values of 7.1 and 580 nM for human recombinant receptors transfected into HEK and CHO cells, respectively, in a radioligand binding assay. It is considered a protean agonist as it has neutral antagonist and partial agonist activity, depending on the assay utilized. It is also acts in a species-dependent manner in vitro, acting as an agonist at human CB₂ receptors (EC₅₀ = 190 nM) but an inverse agonist at rat and mouse CB₂ receptors (EC₅₀s = 216 and 463 nM, respectively). AM1241 produces antinociception to thermal stimuli in rat hindpaw. The antinociceptive actions of AM1241 were blocked by the CB₂ receptor-selective antagonist AM630 but not by the CB₁ receptor-selective antagonist AM251 . AM1241 is neuroprotective, preventing HIV-1 glycoprotein Gp120-induced apoptosis in primary human and murine neural progenitor cells and increasing cell survival and differentiation. It increases hippocampal neurogenesis and decreases astro- and gliogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days. AM1241 also delays motor impairment in a murine model of amytrophic lateral sclerosis (ALS).
Verwenden
(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.
Verwenden
(2-Iodo-5-nitrophenyl)[1-[(1-methyl-2-piperidinyl)methyl]-1H-indol-3-yl]methanone is a compound from the aminkalkylindole family which exerts potent and selective agonist activity for the cannabinoid receptor CB2.
Biochem/physiol Actions
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.
target
CB2

(R,S)-AM1241 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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