5'-Guanidinonaltrindole (5'-GNTI) is an

opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid us ...

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 ...

used in scientific research which is highly selective for the κ opioid

receptor Receptor may refer to: * Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...

. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist

norbinaltorphimine Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- ...

. It has a slow onset and long duration of action, and produces

antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...

effects in animal studies. It also increases allodynia by interfering with the action of the κ-opioid peptide dynorphin. In addition to activity at the KOR, 5'-GNTI has been found to act as a

positive 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 stimulus. Some of them, like benzodiazepines, are drugs. The site that an allosteric modulator binds to ...

of the α_1A-adrenergic receptor ( EC₅₀ = 41 nM), and this may contribute to its "severe transient effects".

References

Alpha-1 adrenergic receptor agonists Guanidines Indolomorphinans Irreversible antagonists Kappa-opioid receptor antagonists Phenols Semisynthetic opioids Tertiary alcohols {{Analgesic-stub

See also

References