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Dopamine receptor D

1. Function and Regulation: – Dopamine receptor D2 (D2R) is coupled to G protein, inhibiting adenylyl cyclase activity. – Regulation of D2R surface expression by […]

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1. Function and Regulation:
– Dopamine receptor D2 (D2R) is coupled to G protein, inhibiting adenylyl cyclase activity.
– Regulation of D2R surface expression by NCS-1 in mice influences exploration, synaptic plasticity, and memory formation.
– D2R plays roles in fear memory retrieval, discrimination learning, and cognitive flexibility in humans.
– Activation of D2 autoreceptor in flies protects dopamine neurons from cell death.

2. Isoforms and Variants:
– Alternative splicing of the DRD2 gene produces three variants encoding different isoforms.
– Long form (D2Lh) functions post-synaptically, while short form (D2Sh) acts as a pre-synaptic autoreceptor.
– Agonism of D2Sh inhibits dopamine release, while antagonism increases it.
– A third form (D2(Longer)) differs in sequence from the canonical form.

3. Structural Features and Pharmacology:
– D2R exists in active (DHighR) and inactive (DLowR) states crucial for ligand binding and signaling.
– D2R has an orthosteric binding site and a secondary binding pocket essential for allosteric pharmacology.
– Oligomerization of D2R into dimers or higher-order oligomers is supported by experimental evidence.
– Interaction with the secondary binding pocket is necessary for modulators like SB269652.

4. Genetics and Polymorphisms:
– Allelic variants and polymorphisms in the DRD2 gene are associated with disorders like schizophrenia and Parkinson’s disease.
– Specific splice variants in Dopamine receptor D2 are linked to symptoms in schizophrenia.
– The DRD2 TaqIA polymorphism relates to motor fluctuations in Parkinson’s disease.

5. Research Findings and Pharmacological Insights:
– Various studies have explored the role of D2 receptors in cognition, memory, fear response, and synaptic plasticity.
– Genetic markers linked to reduced striatal D2 receptor density have implications for cognitive goal maintenance.
– Pharmacological research has investigated interactions, modulation, and effects of drugs on dopamine D2 receptors.

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