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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 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...
Adrenergic Receptors: β Subtype01:26

Adrenergic Receptors: β Subtype

β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors have equal affinities for...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...
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...

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Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
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Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors

Published on: June 7, 2016

α-Adrenoceptor assays.

Peter W Abel1, Neha Jain

  • 1Department of Pharmacology, Creighton University School of Medicine, Omaha, Nebraska, USA.

Current Protocols in Pharmacology
|December 22, 2012
PubMed
Summary
This summary is machine-generated.

This study details in vitro methods for investigating alpha-adrenoceptor functions and identifying new ligands. Protocols are provided for studying alpha-1 and alpha-2 adrenoceptor subtypes using isolated tissues.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Physiology

Background:

  • Alpha-adrenoceptors modulate sympathetic nerve and central noradrenergic neuron activity.
  • They function as autoreceptors, regulating norepinephrine (NE) and neurotransmitter release.
  • Two main classes, alpha-1 and alpha-2, with six subtypes (α(1A), α(1B), α(1D), α(2A), α(2B), α(2C)) exist.

Purpose of the Study:

  • To describe in vitro isolated tissue methods for studying alpha-adrenoceptor functions.
  • To provide protocols for identifying novel ligands targeting alpha-adrenoceptor subtypes.
  • To facilitate research on the diverse roles of alpha-1 and alpha-2 adrenoceptor subtypes.

Main Methods:

  • Utilizes in vitro isolated tissue preparations.
  • Employs established protocols for functional assays of adrenoceptors.
  • Focuses on subtype-specific investigations of alpha-1 and alpha-2 adrenoceptors.

Main Results:

  • Provides detailed experimental protocols.
  • Enables functional characterization of alpha-adrenoceptor subtypes.
  • Facilitates the discovery and validation of new adrenoceptor ligands.

Conclusions:

  • The described methods are essential for advancing the understanding of alpha-adrenoceptor pharmacology.
  • These protocols support the development of targeted therapeutics by enabling precise ligand identification.
  • This unit serves as a valuable resource for researchers studying adrenoceptor-mediated physiological processes.