PNU-282,987
Encyclopedia
PNU-282,987 is a drug that acts as a potent and selective agonist
for the α7
subtype of neural nicotinic acetylcholine receptor
s. In animal studies, it shows nootropic
effects, and derivatives may be useful in the treatment of schizophrenia
, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG
antitarget
.
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
for the α7
Alpha-7 nicotinic receptor
The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor, consisting entirely of α7 subunits....
subtype of neural nicotinic acetylcholine receptor
Nicotinic acetylcholine receptor
Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...
s. In animal studies, it shows nootropic
Nootropic
Nootropics , also referred to as smart drugs, brain steroids, memory enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration...
effects, and derivatives may be useful in the treatment of schizophrenia
Schizophrenia
Schizophrenia is a mental disorder characterized by a disintegration of thought processes and of emotional responsiveness. It most commonly manifests itself as auditory hallucinations, paranoid or bizarre delusions, or disorganized speech and thinking, and it is accompanied by significant social...
, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG
HERG
hERG is a gene that codes for a protein known as Kv11.1 potassium ion channel...
antitarget
Antitarget
In pharmacology, an antitarget is a receptor, enzyme, or other biological target that, when affected by a drug, causes undesirable side-effects. During drug design and development, it is important for pharmaceutical companies to ensure that new drugs do not show significant activity at any of a...
.