|
|
| | CONESSINE Basic information |
| | CONESSINE Chemical Properties |
| Melting point | 126-127°C | | alpha | D20 +25.3° (c = 0.7 in abs alc) | | Boiling point | 479.38°C (rough estimate) | | density | 0.9492 (rough estimate) | | refractive index | 1.5640 (estimate) | | storage temp. | Store at RT | | solubility | ethanol: ≥2mg/mL | | form | powder | | pka | 10.20±0.70(Predicted) | | color | white to tan | | LogP | 6.060 (est) |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 | | RTECS | GK7621000 | | HS Code | 2939799090 |
| | CONESSINE Usage And Synthesis |
| Description | 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 (Kis = 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. | | Uses | antiamebic, antibacterial, antineoplastic, anesthetic (local) | | Uses | 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. | | Biological Activity | 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). | | Purification Methods | 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.] |
| | CONESSINE Preparation Products And Raw materials |
|