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Related Concept Videos

Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

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 C—inositol-1,4,5-trisphosphate...
Adrenergic Neurons: Neurotransmission01:27

Adrenergic Neurons: Neurotransmission

Postganglionic sympathetic fibers (except those supplying the sweat glands) releasing noradrenaline or norepinephrine are called noradrenergic or adrenergic neurons. Noradrenaline, dopamine, adrenaline, or epinephrine are collectively called "catecholamines" as they contain a catechol moiety and an amine side chain. The five stages of neurotransmitter release involve their synthesis, storage, release, reuptake and metabolism.
Synthesis: Catecholamine synthesis requires tyrosine, which is taken...
Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
Adrenergic Agonists: Indirect-Acting Agents01:25

Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...
Cholinergic Receptors: Nicotinic01:15

Cholinergic Receptors: Nicotinic

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...
Adrenergic Receptors (Adrenoceptors): Classification01:27

Adrenergic Receptors (Adrenoceptors): Classification

Adrenergic receptors, or adrenoceptors, respond to the autonomic neurotransmitter noradrenaline and other endogenous catecholamine agonists. They are classified into two main families, α and β, based on their pharmacological response and are further subdivided depending on their location, elicited response, and affinity to specific agonists or antagonists.
α-Adrenoceptors
α-Adrenoceptors are classified into two main subtypes: α1 and α2. The α1 adrenoceptors, which are found on postsynaptic...

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Related Experiment Video

Updated: Jun 12, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
07:16

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission

Published on: August 16, 2018

Adenosine: The prototypic neuromodulator.

M Williams1

  • 1Research Department, Pharmaceuticals Division, CIBA-Geigy, Summit, NJ 07901, U.S.A.

Neurochemistry International
|May 28, 2010
PubMed
Summary
This summary is machine-generated.

Adenosine acts as a crucial homeostatic neuromodulator in mammals, influencing various physiological systems. Understanding its receptor interactions is key to developing novel therapeutics targeting modulatory, rather than direct transmitter, responses.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • Purinergic modulation in mammals was observed in 1929, but adenosine's ubiquitous nature caused initial skepticism regarding its specific roles.
  • Biochemical studies, spurred by cyclic AMP discovery, identified adenosine as a potential chemical messenger.
  • The discovery of adenosine receptors (A1 and A2) and selective antagonists provided evidence for its involvement in various drug actions.

Purpose of the Study:

  • To elucidate the functional role of adenosine as a chemical messenger and neuromodulator.
  • To investigate adenosine's implication in the pharmacological actions of centrally active agents.
  • To explore adenosine's potential as a prototypic homeostatic neuromodulator.

Main Methods:

  • Biochemical studies to identify adenosine's messenger functions.
  • Pharmacological investigations using selective adenosine receptor antagonists.
  • Analysis of adenosine's effects on various physiological systems.

Main Results:

  • Adenosine is implicated in the action of anxiolytics, antipsychotics, antidepressants, cognitive enhancers, and anticonvulsants.
  • Adenosine exerts potent effects on cardiovascular, pulmonary, renal, and immune functions, with implications for central nervous system (CNS) function.
  • Adenosine functions as a homeostatic neuromodulator, potentially representing a prototypic agent of this class.

Conclusions:

  • Adenosine acts as a significant homeostatic neuromodulator with broad physiological impacts.
  • Targeting adenosine function through novel antagonists offers potential for developing new therapeutic agents.
  • Further research in medicinal chemistry can refine understanding and applications of adenosine modulation.