R6890, sometimes known as spirochlorphine, is an opioid
analgesic
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
and a member of the
spiropiperidine family of agents.
The first known mention of this compound was in 1977.
It has been advertised online as a
research chemical
Research chemicals are chemical substances which scientists use for medical and scientific research purposes. One characteristic of a research chemical is that it is for laboratory research use only; a research chemical is not intended for human ...
having a potency 2-5 times that of fentanyl. Other examples of agents from this class are
Ro64-6198 and
Ro65-6570.
Brorphine
Brorphine is a piperidine-based opioid analgesic compound. Brorphine was originally discovered in a 2018 paper investigating functionally biased opioid compounds, with the intention of finding safer analgesics that produce less respiratory depre ...
also has a similar structure.
A precursor chemical used in the synthesis of R6890 is 1-phenyl-1,3,8-triazaspiro(4,5)decan-4-one (also known as
spirodecanone
Spirodecanone refers to a class of spirocyclic ketones, often studied for their potential applications in medicinal chemistry. One notable example is 1-Phenyl-1,3,8-triazaspiro .5ecan-4-one, which has been investigated as a metabolite of neurol ...
), which is used in the synthesis of other drugs including
spirilene,
fluspirilene,
spiramide,
spiperone
Spiperone, also known as spiroperidol and sold under the brand name Spiropitan (( JP)) is a typical antipsychotic of the butyrophenone family related to haloperidol. It is approved for clinical use in Japan as a treatment for schizophrenia.
Pha ...
,
RP-23618,
spioxatrine,
L008716 and R5260.
Pharmacology
The pharmacology of R6890 is described as a
nociceptin receptor (NOP) agonist, although R6890 retains significant affinity at the
mu opioid receptor.
R6890 has
affinities (K
i values) of 4, 75, and 10 nM for the mu, delta, and the total
opioid receptor
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostati ...
population, respectively.
See also
*
Cychlorphine
Cychlorphine is a chemical compound which has been sold as a designer drug, reported in five European countries since 2024, and in the USA. It is similar in chemical structure to known opioid agonists such as brorphine and spirochlorphine, and is ...
*
List of orphine opioids
References
{{Opioid receptor modulators
Analgesics
Belgian inventions
Euphoriants
Mu-opioid receptor agonists
Piperidines
Synthetic opioids
4-Chlorophenyl compounds
Anilines
Spiro compounds
Imidazolidinones