BD1063 or 1-
-(3,4-dichlorophenyl)ethyl4-methylpiperazine is a selective
sigma receptor antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
, with a reported
binding affinity
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a mol ...
of ''K''
i = 9 ± 1 nM for the
sigma-1 receptor and more than 49 times selectivity over the
sigma-2 receptor
The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as cancer and neurological diseases. It is currently under investigation for its potential diagnostic and therapeutic use ...
.
Consistent with other reported
sigma receptor antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
s, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine.
In other animal studies, BD1063 blocks the effects of
MDMA
3,4-Methylenedioxymethamphetamine (MDMA), commonly seen in Tablet (pharmacy), tablet form (ecstasy) and crystal form (molly or mandy), is a potent empathogen–entactogen with stimulant properties primarily used for Recreational dru ...
,
and reduces alcohol intake in rodent models of
alcoholism
Alcoholism is, broadly, any drinking of alcohol (drug), alcohol that results in significant Mental health, mental or physical health problems. Because there is disagreement on the definition of the word ''alcoholism'', it is not a recognize ...
.
See also
*
BD1008
BD1008 or N- -(3,4-dichlorophenyl)ethylN-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of ''K''i = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor.
...
*
BD1031
BD1031 or (R)-2- -(3,4-dichlorophenyl)ethylctahydropyrrolo ,2-ayrazine is a selective sigma receptor agonist, with a reported binding affinity of ''K''i = 1 ± 0.2 nM for the sigma-1 receptor and 80 times selectivity over the sigma-2 receptor. Th ...
*
LR132
LR132 or (+)-3,4-dichloro-N- 1R,2S)-2-(1-pyrrolidinyl)cyclohexylenzeneethanamine is a selective sigma receptor antagonist, with a reported binding affinity of ''K''i = 2 ± 0.1 nM for the sigma-1 receptor and more than 350 times selectivity over ...
References
{{Sigma receptor modulators
Chloroarenes
Piperazines