Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
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Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
Proc Natl Acad Sci U S A. 1992 Apr 15;89(8):3630-4.
- PubMed ID
- 1565658 [ View in PubMed]
- Abstract
The serotonin 1D (5-HT1D) receptor is a pharmacologically defined binding site and functional receptor site. Observed variations in the properties of 5-HT1D receptors in different tissues have led to the speculation that multiple receptor proteins with slightly different properties may exist. We report here the cloning, deduced amino acid sequences, pharmacological properties, and second-messenger coupling of a pair of human 5-HT1D receptor genes, which we have designated 5-HT1D alpha and 5-HT1D beta due to their strong similarities in sequence, pharmacological properties, and second-messenger coupling. Both genes are free of introns in their coding regions, are expressed in the human cerebral cortex, and can couple to inhibition of adenylate cyclase activity. The pharmacological binding properties of these two human receptors are very similar, and match closely the pharmacological properties of human, bovine, and guinea pig 5-HT1D sites. Both receptors exhibit high-affinity binding of sumatriptan, a new anti-migraine medication, and thus are candidates for the pharmacological site of action of this drug.
DrugBank Data that Cites this Article
- Polypeptides
Name UniProt ID 5-hydroxytryptamine receptor 1D P28221 Details 5-hydroxytryptamine receptor 1B P28222 Details - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Methysergide 5-hydroxytryptamine receptor 1B Ki (nM) 3.6 N/A N/A Details Pindolol 5-hydroxytryptamine receptor 1B Ki (nM) 4100 N/A N/A Details Sumatriptan 5-hydroxytryptamine receptor 1B Ki (nM) 3.4 N/A N/A Details Sumatriptan 5-hydroxytryptamine receptor 1D Ki (nM) 7.7 N/A N/A Details Yohimbine 5-hydroxytryptamine receptor 1B Ki (nM) 16 N/A N/A Details Yohimbine 5-hydroxytryptamine receptor 1B Ki (nM) 22 N/A N/A Details Yohimbine 5-hydroxytryptamine receptor 1D Ki (nM) 40 N/A N/A Details Yohimbine 5-hydroxytryptamine receptor 1D Ki (nM) 27 N/A N/A Details