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α1D-adrenoceptor
Previous and Unofficial Names  |
| α1a/d-adrenoceptor |
| α1A-adrenoceptor |
| adrenergic receptor |
Structural Information  |
|
class A G protein-coupled receptor |
| Species |
TM |
AA |
Chromosomal Location |
Gene Name |
Reference |
| Human |
7 |
572 |
20p13 |
ADRA1D
|
47 |
| Rat |
7 |
561 |
3q36 |
Adra1d
|
32 |
| Mouse |
7 |
562 |
2 F1 |
Adra1d
|
30 |
|
|
Database Links  |
|
ChEMBL Target |
103 (Hs), 10646 (Mm), 12742 (Rn) |
|
Ensembl |
ENSG00000171873 (Hs), ENSMUSG00000027335 (Mm), ENSRNOG00000021256 (Rn) |
|
Entrez Gene |
146 (Hs), 11550 (Mm), 29413 (Rn) |
|
GeneCards |
ADRA1D (Hs) |
|
OMIM |
104219 (Hs) |
|
PharmGKB Gene |
PA24597 (Hs) |
|
Protein Ontology (PRO) |
PRO:000001185 (Hs) |
|
RefSeq Nucleotide |
NM_000678 (Hs), NM_013460 (Mm), NM_024483 (Rn) |
|
RefSeq Protein |
NP_000669 (Hs), NP_038488 (Mm), NP_077809 (Rn) |
|
UniGene Hs. |
557 (Hs) |
|
UniProt |
P25100 (Hs), P97714 (Mm), P23944 (Rn) |
|
Wikipedia |
α1D-adrenoceptor |
| Search for 3D structures on the PDB |
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Search using keywords: Adrenoceptors alpha1D-adrenoceptor
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Search using accession numbers: P23944 || P25100 || P97714
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| Antagonists |
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Key to terms and symbols
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View all chemical structures |
Click column headers to sort
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View species-specific antagonist tables
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| Antagonist Comments |
Although cyslazosin does not show selectivity in radioligand binding assays with recombinant α1-adrenoceptors, functional selectivity for the α1D-adrenoceptor is observed in functional assays using isolated tissue assays measuring affinity for native α1- subtypes [49].
Differentiation between neutral antagonists and inverse agonists at the α1D- adrenoceptor has not been studied extensively. |
| Allosteric Regulator Comments |
| Lorazepam and midazolam have been shown to increase the maximum response to phenylephrine in cells expressing the human α1D-adrenoceptor[48]. |
Primary Transduction Mechanisms
|
| Transducer |
Effector/Response |
|
Gq/G11 family |
Phospholipase C stimulation Calcium channel Other - See Comments |
Secondary Transduction Mechanisms  |
| Transducer |
Effector/Response |
|
|
Phospholipase D stimulation Other - See Comments |
Tissue Distribution
|
| α1D- adrenoceptor message and protein is predominant in human bladder. |
| Species: |
Human |
| Technique: |
RNase protection assay, RT-PCR. |
| References: |
50 |
|
|
| In the rat brain, highest levels of α1D-adrenoceptor message are found in the olfactory bulb, cerebral cortex, hippocampus, dentate gyrus, reticular thalamic nucleus, motor neurons and the inferior olivary complex. In the thalamus, the α1B and α1D-adrenoceptors have a complimentary distribution. |
| Species: |
Rat |
| Technique: |
in situ hybridisation. |
| References: |
58 |
|
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| The α1D-adrenoceptor was the predominant α1 subtype in the human aorta, but either had the lowest expression of the three subtypes, or was not detectable, in other arteries and veins. However, another report showed high expression of α1D-adrenoceptor in blood vessels of human prostate. |
| Species: |
Human |
| Technique: |
RNAse Protection, immunohistochemistry. |
| References: |
11,59 |
|
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Functional Assays
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| Isolated rat aortic ring. |
| Species: |
Rat |
| Tissue: |
Vasculature. |
| Response measured: |
Contraction. |
| References: |
56 |
|
|
| Skeletal muscle arteriole. |
| Species: |
Rat |
| Tissue: |
Vasculature. |
| Response measured: |
Contraction. |
| References: |
57 |
|
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Physiological Functions
|
| Contraction of mesenteric resistance arteries. |
| Species: |
Rat |
| Tissue: |
Vasculature. |
| References: |
5 |
|
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| α1D-adrenoceptors mediate nerve stimulated contraction of corpus cavernosa. |
| Species: |
Rat |
| Tissue: |
Corpus Cavernosa. |
| References: |
60 |
|
|
| Coronary artery vasoconstriction. |
| Species: |
Mouse |
| Tissue: |
Vasculature. |
| References: |
41 |
|
|
| Femoral artery vasoconstriction. |
| Species: |
Rat |
| Tissue: |
Vasculature. |
| References: |
61 |
|
|
| Locomotor activity in response to environmental stimulation. |
| Species: |
Mouse |
| Tissue: |
Brain. |
| References: |
62 |
|
|
| Reflex evoked urethral contraction. |
| Species: |
Rat |
| Tissue: |
Urethra. |
| References: |
63 |
|
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| Endothelium dependent vasodilation of mesenteric vascular bed. |
| Species: |
Rat |
| Tissue: |
Vasculature. |
| References: |
64 |
|
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Physiological Consequences of Altering Gene Expression
|
| α1D knockout mice had delayed tail-flick and hindpaw-licking responses to thermal stimuli. |
| Species: |
Mouse |
| Tissue: |
|
| Technique: |
Transgenesis. |
| References: |
53 |
|
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| α1D knockout mice had hypotension, a decreased pressor and decreased coronary vasoconstrictor response to phenylephrine and resistance to salt induced hypertension. |
| Species: |
Mouse |
| Tissue: |
|
| Technique: |
Transgenesis. |
| References: |
41,54-55 |
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Receptor Comments |
α1D- adrenoceptor message and protein is predominant in human bladder [50]. In bladder tissue from normal rats, only 25% of α1- adrenoceptor message was of the α1D- subtype; however following bladder obstruction, this percentage increased to 75% [51].
When recombinant α1D- adrenoceptors are expressed in fibroblast cell lines, most of the expression is intracellular, as opposed to the cell surface expression of the other α1 subtypes [52]. |
To cite this receptor data page, please use the following:
Richard A. Bond, David B. Bylund, Douglas C. Eikenburg, J. Paul Hieble, Rebecca Hills, Kenneth P. Minneman, Sergio Parra.
Adrenoceptors: α1D-adrenoceptor. Last modified on 2010-06-28. Accessed on 2010-09-03. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=24.
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