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Related Concept Videos

Cholinergic Receptors: Nicotinic01:15

Cholinergic Receptors: Nicotinic

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Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
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Cholinergic Receptors: Muscarinic01:25

Cholinergic Receptors: Muscarinic

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The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine. 
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
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Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

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Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
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Indirect-Acting Cholinergic Agonists: Pharmacological Actions01:30

Indirect-Acting Cholinergic Agonists: Pharmacological Actions

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Indirect-acting cholinergic agonists, also known as anticholinesterases, exert their pharmacological effects by enhancing cholinergic transmission in various body parts, including the neuromuscular junction, autonomic cholinergic synapses, and the brain.
At the neuromuscular junction, these agents work by inhibiting the breakdown of acetylcholine, allowing it to remain bound to the receptor and bind to nearby receptors. This process leads to repetitive firing of the endplate, causing muscle...
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Indirect-Acting Cholinergic Agonists: Mechanism of Action01:18

Indirect-Acting Cholinergic Agonists: Mechanism of Action

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Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
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Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

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Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Imidazoline I2 receptors: An update.

Jun-Xu Li1

  • 1School of Pharmacy, Nantong University, Nantong, Jiangsu Province, China; Department of Pharmacology and Toxicology, Jacobs School of Medicine and Biomedical Sciences, University at Buffalo, Buffalo, New York, USA.

Pharmacology & Therapeutics
|March 22, 2017
PubMed
Summary

Research on imidazoline I2 receptors is growing, with ligands showing promise for chronic pain relief. One drug, CR4056, is in clinical trials for osteoarthritis, highlighting I2 receptors as a potential target for neurological disorders.

Keywords:
Body temperatureDrug discriminationImidazoline I(2) receptorNeuroprotectionPain

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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
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Spectral Confocal Imaging of Fluorescently tagged Nicotinic Receptors in Knock-in Mice with Chronic Nicotine Administration
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Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Discovery

Background:

  • Imidazoline I2 receptors, also known as I2 binding sites, interact with specific ligands like [3H]-idazoxan and [3H]-2-BFI.
  • The precise molecular identities of the proteins constituting I2 receptors are still under investigation, though one 45kD protein may be brain creatine kinase.

Purpose of the Study:

  • To review the current state of I2 receptor pharmacology.
  • To highlight the therapeutic potential of I2 receptor ligands for various neurological conditions.

Main Methods:

  • Review of existing literature on I2 receptor ligands and their biological effects.
  • Analysis of preclinical and clinical data for selective I2 receptor modulators.

Main Results:

  • Selective I2 receptor ligands demonstrate efficacy in treating persistent pain conditions, including inflammatory, neuropathic, and postoperative pain.
  • CR4056, a selective I2 receptor ligand, has progressed to Phase II clinical trials for chronic inflammatory pain (osteoarthritis).
  • I2 receptor ligands exhibit neuroprotective effects, modulate body temperature, and possess discriminative stimulus activity in animal models.

Conclusions:

  • I2 receptors represent a promising drug target for neurological disorders, particularly pain and stroke.
  • Further research is needed to translate preclinical findings into effective pharmacotherapies for conditions like chronic pain and neurodegeneration.