A1APU (10105-368-30-605-0) is a
negative allosteric modulator
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or alcohol, function as psychoactive drugs. The site that a ...
(NAM) of the
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...
(MOR) which has been developed as a potential treatment for
opioid overdose
An opioid overdose is toxicity due to excessive consumption of opioids, such as morphine, codeine, heroin, fentanyl, tramadol, and methadone. This preventable pathology can be fatal if it leads to respiratory depression, a lethal conditio ...
. In animal studies it increases the potency and effective duration of
naloxone
Naloxone, sold under the brand name Narcan among others, is an opioid antagonist, a medication used to reverse or reduce the effects of opioids. For example, it is used to restore breathing after an opioid overdose. Effects begin within two ...
making it able to block opioid-induced
respiratory depression
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapni ...
at a tenth of the normal dose.
See also
*
MS1 (drug)
MS1 is a positive allosteric modulator (PAM) of the μ-opioid receptor (MOR). It was developed from structural modification of the earlier MOR PAM BMS‐986122.
The drug has been found to augment the affinity (pharmacology), affinity of the MOR ...
References
{{Opioid receptor modulators
Experimental drugs
Benzyl compounds
Pyridines
Naphthalenes
Thioethers
Carboxamides
Methoxyphenethylamines