Abstract
The cholinergic activity in the brain is fundamental for cognitive functions. The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Accumulating evidence indicates that both nAChR and mAChRs can modulate the release of several other neurotransmitters, modify the threshold of long-term plasticity, finally improving learning and memory processes. Importantly, the expression, distribution, and/or function of these systems are altered in several neurological diseases. The aim of this review is to discuss our current knowledge on cholinergic receptors and their regulating synaptic functions and neuronal network activities as well as their use as targets for the development of new and clinically useful cholinergic ligands. These new therapies involve the development of novel and more selective cholinergic agonists and allosteric modulators as well as selective cholinesterase inhibitors, which may improve cognitive and behavioral symptoms, and also provide neuroprotection in several brain diseases. The review will focus on two nAChR receptor subtypes found in the mammalian brain and the most commonly targeted in drug discovery programs for neuropsychiatric disorder, the ligands of α4β2 nAChR and α7 nAChRs.
| Original language | English |
|---|---|
| Pages (from-to) | 2004-2014 |
| Number of pages | 11 |
| Journal | Current Pharmaceutical Design |
| Volume | 22 |
| Issue number | 14 |
| DOIs | |
| State | Published - 1 Apr 2016 |
| Externally published | Yes |
Fingerprint
Keywords
- Acetylcholine
- Muscarinic receptors
- Neurological disease
- Nicotinic receptors
- Synaptic plasticity
Cite this
}
Role of nicotinic and muscarinic receptors on synaptic plasticity and neurological diseases. / Fuenzalida, Marco; Pérez, Miguel Ángel; Arias, Hugo R.
In: Current Pharmaceutical Design, Vol. 22, No. 14, 01.04.2016, p. 2004-2014.Research output: Contribution to journal › Article
TY - JOUR
T1 - Role of nicotinic and muscarinic receptors on synaptic plasticity and neurological diseases
AU - Fuenzalida, Marco
AU - Pérez, Miguel Ángel
AU - Arias, Hugo R.
PY - 2016/4/1
Y1 - 2016/4/1
N2 - The cholinergic activity in the brain is fundamental for cognitive functions. The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Accumulating evidence indicates that both nAChR and mAChRs can modulate the release of several other neurotransmitters, modify the threshold of long-term plasticity, finally improving learning and memory processes. Importantly, the expression, distribution, and/or function of these systems are altered in several neurological diseases. The aim of this review is to discuss our current knowledge on cholinergic receptors and their regulating synaptic functions and neuronal network activities as well as their use as targets for the development of new and clinically useful cholinergic ligands. These new therapies involve the development of novel and more selective cholinergic agonists and allosteric modulators as well as selective cholinesterase inhibitors, which may improve cognitive and behavioral symptoms, and also provide neuroprotection in several brain diseases. The review will focus on two nAChR receptor subtypes found in the mammalian brain and the most commonly targeted in drug discovery programs for neuropsychiatric disorder, the ligands of α4β2 nAChR and α7 nAChRs.
AB - The cholinergic activity in the brain is fundamental for cognitive functions. The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Accumulating evidence indicates that both nAChR and mAChRs can modulate the release of several other neurotransmitters, modify the threshold of long-term plasticity, finally improving learning and memory processes. Importantly, the expression, distribution, and/or function of these systems are altered in several neurological diseases. The aim of this review is to discuss our current knowledge on cholinergic receptors and their regulating synaptic functions and neuronal network activities as well as their use as targets for the development of new and clinically useful cholinergic ligands. These new therapies involve the development of novel and more selective cholinergic agonists and allosteric modulators as well as selective cholinesterase inhibitors, which may improve cognitive and behavioral symptoms, and also provide neuroprotection in several brain diseases. The review will focus on two nAChR receptor subtypes found in the mammalian brain and the most commonly targeted in drug discovery programs for neuropsychiatric disorder, the ligands of α4β2 nAChR and α7 nAChRs.
KW - Acetylcholine
KW - Muscarinic receptors
KW - Neurological disease
KW - Nicotinic receptors
KW - Synaptic plasticity
UR - http://www.scopus.com/inward/record.url?scp=84969142070&partnerID=8YFLogxK
U2 - 10.2174/1381612822666160127112021
DO - 10.2174/1381612822666160127112021
M3 - Article
C2 - 26818867
AN - SCOPUS:84969142070
VL - 22
SP - 2004
EP - 2014
JO - Current Pharmaceutical Design
JF - Current Pharmaceutical Design
SN - 1381-6128
IS - 14
ER -