Conessin

Bezeichnung:Conessin

CAS-Nr546-06-5

Englisch Name:CONESSINE

CBNumberCB8139148

SummenformelC24H40N2

Molgewicht356.59

MOL-Datei546-06-5.mol

Synonyma

Conessin

Conessin physikalisch-chemischer Eigenschaften

Schmelzpunkt	126-127°C
alpha	D20 +25.3° (c = 0.7 in abs alc)
Siedepunkt	479.38°C (rough estimate)
Dichte	0.9492 (rough estimate)
Brechungsindex	1.5640 (estimate)
storage temp.	Store at RT
Löslichkeit	ethanol: ≥2mg/mL
Aggregatzustand	powder
pka	10.20±0.70(Predicted)
Farbe	white to tan
Optische Aktivität	+25.320 (c 0.7, ethanol)
LogP	6.060 (est)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3
RTECS-Nr.	GK7621000
HS Code	2939799090

Gefahreninformationscode (GHS)

CONESSINE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Conessine is a naturally occurring steroid alkaloid found in a number of plant species from the Apocynaceae family, which have been used in traditional herbal medicine as a treatment for amoebic dysentery. In a radioligand-based high-throughput screen, conessine demonstrated high affinity for both rat and human histamine H3 receptors (K_is = 5.2 and 24.5 nM, respectively) and high selectivity against histamine receptors H1, H2, and H4. Though conessine potently blocks H3 agonist-stimulated GTPγS binding in cell- and tissue-based functional assays and efficiently crosses the blood-brain barrier, it has a poor rate of CNS clearance.
Verwenden
antiamebic, antibacterial, antineoplastic, anesthetic (local)
Verwenden
Conessine is a steroidal dibasic alkaloid with a rigid steroid-based skeleton. Conessine is a potent and selective histamine H3 receptor antagonist.
Definition
ChEBI: A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae.
Biologische Aktivität
Potent and selective histamine H 3 receptor antagonist (pK i values are 7.61 and 8.27 at rat and human H 3 receptors respectively). A steroidal alkaloid that displays in vitro antiplasmodial activity (IC 50 = 1.04 μ M). Also has high affinity for α 2C adrenoceptors (pK i = 7.98).
läuterung methode
It crystallises from acetone, sublimes at 95o/0.01mm and boils at 0.1mm with bath temperature at 220o. The dihydrochloride has m >340o (browns at 235o and decomposes at 338-240o) and has [] D +9.3o (c 2, H2O). [Marshall & Johnson J Am Chem Soc 84 1458 1962, Beilstein 22 III/IV 4382.]

Conessin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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