AM-694 (1-(5-fluoropentyl)-3-(2-iodobenzoyl)indole) is a
designer drug that acts as a potent and selective
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
for the
cannabinoid receptor CB1. It is used in scientific research for mapping the distribution of CB
1 receptors.
Pharmacology
AM-694 is an
agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
for
cannabinoid receptors. It has a
''K''i of 0.08 nM at
CB1 and 18 times selectivity over
CB2 with a ''K''
i of 1.44 nM.
It is unclear what is responsible for this unusually high CB
1 binding affinity, but it makes the
18F radiolabelled derivative of AM-694 useful for mapping the distribution of CB
1 receptors in the body.
[
]
Metabolism
Pathways of metabolism
Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the co ...
include hydrolytic
Hydrolysis (; ) is any chemical reaction in which a molecule of water breaks one or more chemical bonds. The term is used broadly for substitution, elimination, and solvation reactions in which water is the nucleophile.
Biological hydrolysis ...
defluorination, carboxylation, and monohydroxylation of the ''N''-alkyl chain.
See also
* AM-679
* AM-1235
* AM-2201
* AM-2232
* AM-2233
* FUBIMINA
FUBIMINA (also known as BIM-2201, BZ-2201 and FTHJ) is a synthetic cannabinoid that is the benzimidazole structural analog, analog of AM-2201 and has been used as an active ingredient in synthetic cannabis products. It was first identified in J ...
* JWH-018
* List of AM cannabinoids
* List of JWH cannabinoids
* THJ-2201
THJ-2201 is an indazole-based synthetic cannabinoid that presumably acts as a potent agonist of the CB1 receptor, CB1 receptor and has been sold online as a designer drug.
It is a structural analog of AM-2201 in which the central indole ring h ...
References
{{Cannabinoids
Benzoylindoles
2-Iodophenyl compounds
Organofluorides
AM cannabinoids
Designer drugs
PET radiotracers