Rolipram

Bezeichnung:Rolipram

CAS-Nr61413-54-5

Englisch Name:ROLIPRAM

CBNumberCB2703866

SummenformelC16H21NO3

Molgewicht275.34

MOL-Datei61413-54-5.mol

Synonyma

Rolipram

Rolipram physikalisch-chemischer Eigenschaften

Schmelzpunkt	127-133 °C
Siedepunkt	418.29°C (rough estimate)
Dichte	1.0677 (rough estimate)
Brechungsindex	1.5500 (estimate)
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	H₂O: 0.2 mg/mL
Aggregatzustand	solid
pka	16.02±0.40(Predicted)
Farbe	white to off-white
Merck	14,8251
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38-11
S-Sätze:	26-36
RIDADR	3249
WGK Germany	3
RTECS-Nr.	UY5749237
HazardClass	6.1(b)
PackingGroup	III
HS Code	29337900
Toxizität	LD50 oral in mouse: > 300mg/kg

Gefahreninformationscode (GHS)

ROLIPRAM Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Rolipram (61413-54-5) is a selective inhibitor of cAMP-specific phosphodiesterase (PDE4), IC50 = 1 μM. Displays beneficial effects in neurodegenerative diseases. Rolipram also displays anti-inflammatory activity and synergizes with forskolin (cat.# 10-2073). Cell permeable.
Chemische Eigenschaften
Yellowish solid
Verwenden
(±)-Rolipram is a cAMP-specific phosphodiesterase 4 (PDE4) inhibitor.
Verwenden
Pharmacological tool for characterization of phosphodiesterase isoenzymes.
Verwenden
A selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4).
Verwenden
antipsychotic
Definition
ChEBI: Rolipram is a member of the lclass of pyrrolidin-2-ones that is pyrrolidin-2-one bearing a 3-(cyclopentyloxy)-4-methoxyphenyl substituent at the 4-position. It is a type IV-specific phosphodiesterase (PDE4) inhibitor. It has a role as an antidepressant and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor.
Allgemeine Beschreibung
A cell-permeable, selective inhibitor of cAMP-specific phosphodiesterase (PDE IV; IC₅₀ = 800 nM). A rolipram-insensitive PDE IV subtype is also known to exist. Also inhibits NF-κB and NFAT activation in Jurkat and primary T cells.
Biologische Aktivität
Selective inhibitor of cAMP phosphodiesterase (PDE4) (IC 50 = 2.0 μ M). Discriminates between two conformational states of PDE4 isoenzymes. See separate isomers ((R)-(-)-Rolipram and (S)-(+)-Rolipram).
Biochem/physiol Actions
Cell permeable: yes
Lager
Room temperature
Einzelnachweise
1) Reeves et al. (1987), The identification of a new cyclic nucleotide phosphodiesterase activity in human and guinea-pig cardiac ventricle. Implications for the mechanism of action of selective phosphodiesterase; Biochem. J., 241 535 2) Nishi et al. (2008), Distinct Roles of PDE4 and PDE10A in the Regulation of cAMP/PKA Signaling in the Striatum; J. Neurosci., 28 10460 3) Christiansen et al. (2011), Combined anti-inflammatory effects of β2-adrenergic agonists and PDE4 inhibitors on astrocytes by upregulation of intracellular cAMP; Neurochem. Int., 59 837

Rolipram Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

61413-54-5, ROLIPRAM Verwandte Suche:

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