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A receptor autoradiographic and in situ hybridization analysis of the distribution of the 5‐ht7 receptor in rat brain
The distribution of the 5‐ht7 receptor and its mRNA is suggestive of multiple roles for this novel 5‐HT receptor, within several brain systems, and the limbic system (centromedial amygdala, anterior hippocampal rudiment, hypothalamus) is particularly well‐represented, indicating a potential role for the 5-ht7 receptors in affective processes.
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
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.
Multiple subtypes of serotonin receptors are expressed in rat sensory neurons in culture.
The identification of multiple subtypes of serotonin receptors expressed in cultured embryonic sensory neurons suggests that DRG neuronal cultures may be an excellent model to examine the direct effects of serotonin on the activity of these sensory neurons.
5‐HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigs
The potency of agonists in inhibiting adenylate cyclase in cells transfected with human 5-HT1F receptor was also highly correlated with their potency in the animal model of migraine, suggesting that the 5- HT1F receptors is a rational target for migraine therapeutics.
Functional characterization of the recombinant human 5-hydroxytryptamine7(a) receptor isoform coupled to adenylate cyclase stimulation.
Clonal cell lines stably expressing h5-HT7 receptor isoforms will serve as valuable cellular models to study their function and regulation, as well as assist in the development of selective 5- HT7 receptor agents to uncover the biological roles and potential therapeutic applications of this novel receptor subtype.
LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery.
The ability of LY215840 to block the relaxant 5- HT receptor in canine coronary artery may reflect its 5-HT7 receptor antagonist activity and make it a useful tool to probe the relationship between the 5-Hat7 receptor and the coronary vasoactive properties of 5-ht.
Differences in ligand binding profiles between cloned rabbit and human 5-HT1D alpha and 5-HT1D beta receptors: ketanserin and methiothepin distinguish rabbit 5-HT1D receptor subtypes.
Cloned 5-HT1D alpha and 5- HT1D beta receptor subtypes from the rabbit were cloned and their pharmacological profiles evaluated using radioligand binding assays to suggest that 5-Hat1D-mediated responses in rabbit preparations may provide information relevant to the pharmacology of the 5-ht1D receptor subtype in humans.