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CONESSINE

CAS No.
546-06-5
Chemical Name:
CONESSINE
Synonyms
NERIINE;NERVINE;CONESSIN;Konessin;CONESSINE;WRIGHTINE;ROQUESSINE;ROGUESSINE;NSC 119994;Conessinum
CBNumber:
CB8139148
Molecular Formula:
C24H40N2
Molecular Weight:
356.59
MDL Number:
MFCD00016752
MOL File:
546-06-5.mol
MSDS File:
SDS
Last updated:2023-06-08 09:02:07

CONESSINE 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)
FDA UNII EZ38J9BBDF

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P305+P351+P338
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26
WGK Germany  3
RTECS  GK7621000
HS Code  2939799090
NFPA 704
0
2 0

CONESSINE price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0095 Conessine ≥97% (HPLC) 546-06-5 10mg $53.4 2024-03-01 Buy
Sigma-Aldrich SML0095 Conessine ≥97% (HPLC) 546-06-5 50mg $193 2024-03-01 Buy
Cayman Chemical 11700 Conessine ≥98% 546-06-5 50mg $120 2024-03-01 Buy
Cayman Chemical 11700 Conessine ≥98% 546-06-5 100mg $228 2024-03-01 Buy
Cayman Chemical 11700 Conessine ≥98% 546-06-5 250mg $504 2024-03-01 Buy
Product number Packaging Price Buy
SML0095 10mg $53.4 Buy
SML0095 50mg $193 Buy
11700 50mg $120 Buy
11700 100mg $228 Buy
11700 250mg $504 Buy

CONESSINE Chemical Properties,Uses,Production

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

Raw materials

Preparation Products

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3-beta-(dimethylamino)-con-5-enin 3-beta-(dimethylamino)con-5-enine n,18-dihydrotrimethyl-conkurchin n-dimethyl-(3-beta)-con-5-enin-3-amin WRIGHTINE NERVINE NERIINE ROGUESSINE ROQUESSINE CONESSIN CONESSINE (3-BETA)-N,N-DIMETHYL-CON-5-ENIN-3-AMINE 5-CONENIN-3BETA-DIMETHYLAMINE CONESSINE(RG) N,N-Dimethyl-con-5-enin-3-amine CONESSINE(P) (3β)-N,N-dimethyl-con-5-enin-3-amine NSC 119994 Conessine (Wrightine Roguessine) Con-5-enin-3-amine, N,N-dimethyl-, (3β)- Conessinum Konessin Con-5-enin-3-amine,N,N-dimethyl-, (3b)- inhibit,Parasite,Inhibitor,malarial,infection,histamine H3 receptor,Conessine,Histamine Receptor conessine ( or ) Neriine 546-06-5 546-06-7 C24H40N2 Intermediates & Fine Chemicals Pharmaceuticals Steroids