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HomeProduct name listCONESSINE

CONESSINE

Synonym(s):(3β)-N,N-dimethyl-con-5-enin-3-amine;Conessin;Neriine;Roquessine;Wrightine

  • CAS NO.:546-06-5
  • Empirical Formula: C24H40N2
  • Molecular Weight: 356.59
  • MDL number: MFCD00016752
  • EINECS: 208-897-2
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-19 23:02:33
CONESSINE Structural

What is CONESSINE?

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.

The Uses of CONESSINE

Conessine is a steroidal dibasic alkaloid with a rigid steroid-based skeleton. Conessine is a potent and selective histamine H3 receptor antagonist.

The Uses of CONESSINE

antiamebic, antibacterial, antineoplastic, anesthetic (local)

What are the applications of Application

Conessine is a selective antagonist at the histamine H3-receptor

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.]

Properties of CONESSINE

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
pka 10.20±0.70(Predicted)
form  powder
color  white to tan

Safety information for CONESSINE

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for CONESSINE

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