A naturally occurring steroid alkaloid that acts as a potent histamine H3 receptor antagonist (Kis = 5.2 and 24.5 nM for rat and human

Conessine – 50 mg

Brand:
Cayman
CAS:
546-06-5
Storage:
-20
UN-No:
Non-Hazardous - /

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.{21126} 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.{21126}  

 

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Description

A naturally occurring steroid alkaloid that acts as a potent histamine H3 receptor antagonist (Kis = 5.2 and 24.5 nM for rat and human, respectively) that efficiently crosses the blood-brain barrier but has a poor rate of CNS clearance

Formal name: N,N-dimethyl-con-5-enin-3β-amine

Synonyms:  Neriine|NSC 119994|Roquessine|Wrightine

Molecular weight: 356.6

CAS: 546-06-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Natural Products|Alkaloids||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation

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