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GABAB receptor

GABAB receptor is a biology topic covered in the lgStudy science library. This page brings together a partial reference excerpt, illustrations, worked examples, real-world applications and a short study plan, so you can understand GABAB receptor rather than just read about it. In short: GABAB receptors (GABABR) are G-protein coupled receptors for gamma-aminobutyric acid (GABA). GABAB receptors are found in the central nervous system and the autonomic division of the peripheral nervous system.

GABAB receptor — main illustration
GABAB receptor — illustration

Key takeaways

  • GABAB receptor belongs to biology; place it in that map before memorising details.
  • Learn the definition first, then one example that makes the definition concrete.
  • Connect GABAB receptor to a quantity you can measure, compute or draw — that is where exam questions come from.
  • Reproduce the core statement of GABAB receptor from memory before moving on to harder problems.

Reference excerpt

GABAB receptors (GABABR) are G-protein coupled receptors for gamma-aminobutyric acid (GABA). GABAB receptors are found in the central nervous system and the autonomic division of the peripheral nervous system. The receptors were first named in 1981 when their distribution in the CNS which was determined by Norman Bowery and his team using radioactively labelled baclofen.

Functions GABABRs stimulate the opening of K+ channels, specifically GIRKs, which brings the neuron closer to the equilibrium potential of K+. This reduces the frequency of action potentials which reduces neurotransmitter release. Thus GABAB receptors are usually considered as inhibitory receptors. GABAB receptors can also function as an excitatory receptor and facilitate neurotransmitter release via increasing the activity of CaV2.3 channels. GABAB receptors usually reduces the activity of adenylyl cyclase and Ca2+ channels by using G-proteins with Gi/G0 α subunits. GABAB receptors are involved in behavioral actions of ethanol, gamma-hydroxybutyric acid (GHB), baclofen, and possibly in pain. Recent research suggests that these receptors may play an important developmental role.

Structure GABAB receptors are similar in structure to and in the same receptor family with metabotropic glutamate receptors. There are two subunits of the receptor, GABAB1 and GABAB2, and these appear to assemble as obligate heterodimers in neuronal membranes by linking up by their intracellular C termini. In the mammalian brain, two predominant, differentially expressed isoforms of the GABAB1 are transcribed from the Gabbr1 gene, GABAB(1a) and GABAB(1b), which are conserved in different species including humans. This might potentially offer more complexity in terms of the function due to different composition of the receptor. Cryo-electron microscopy structures of the full length GABAB receptor in different conformational states from inactive apo to fully active have been obtained. Unlike Class A and B GPCRs, phospholipids bind within the transmembrane bundles and allosteric modulators bind at the interface of GABAB1 and GABAB2 subunits.

Ligands

Agonists GABA Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy. gamma-Hydroxybutyrate (GHB) Phenibut 4-Fluorophenibut Isovaline 3-Aminopropylphosphinic acid Lesogaberan SKF-97541: 3-Aminopropyl(methyl)phosphinic acid, 10× more potent than baclofen as GABAB agonist, but also GABAA-ρ antagonist Taurine CGP-44532

Positive allosteric modulators ADX71441 ASP-8062 CGP-7930 BHFF Fendiline BHF-177 BSPP GS-39783 INDV-1000

Antagonists Homotaurine Ginsenosides 2-Hydroxysaclofen Saclofen Phaclofen SCH-50911 2-Phenethylamine CGP-35348 CGP-52432: 3-([(3,4-Dichlorophenyl)methyl]amino]propyl) diethoxymethyl)phosphinic acid, CAS# 139667-74-6 CGP-55845: (2S)-3-([(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl)(phenylmethyl)phosphinic acid, CAS# 149184-22-5 SGS-742

See also GABA receptor GABAA receptor

References

External links

Illustrations

GABAB receptor: Lesogaberan
Lesogaberan
GABAB receptor: CGP-7930
CGP-7930
GABAB receptor: Phaclofen
Phaclofen
GABAB receptor: SCH-50911
SCH-50911

Worked examples

Example 1 — a first encounter with GABAB receptor

Start with the simplest possible case. Write down what GABAB receptor claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In biology, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to GABAB receptor before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about GABAB receptor ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of GABAB receptor

In research
GABAB receptor appears in biology research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry
Engineering practice reuses GABAB receptor in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom
GABAB receptor is common in secondary-school and first-year university syllabi. It links to neighbouring topics GABA, G protein-coupled receptors, Genes on human chromosome 6, so understanding it makes those chapters shorter.
In everyday life
Look for GABAB receptor outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.
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How to study GABAB receptor in 20 minutes

  1. Read the reference excerpt below once, without taking notes.
  2. Close the page and write down what GABAB receptor means in your own words.
  3. Compare your version with the excerpt and mark what you missed.
  4. Work through the three examples above with pen and paper.
  5. Explain GABAB receptor out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is GABAB receptor in simple terms?

GABAB receptors (GABABR) are G-protein coupled receptors for gamma-aminobutyric acid (GABA). GABAB receptors are found in the central nervous system and the autonomic division of the peripheral nervous system.

Why does GABAB receptor matter?

Because it connects several biology ideas at once: it gives you a definition you can apply, a quantity you can calculate, and a way to check whether a result is plausible.

How should I study GABAB receptor?

Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

What does this page cover?

It gives you a compact reference excerpt plus original lgStudy explanations, examples, applications and study material on GABAB receptor.

Tags

  • GABA
  • G protein-coupled receptors
  • Genes on human chromosome 6
  • Genes on human chromosome 9

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