5-HT1 Receptor

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Uwe Reuter - One of the best experts on this subject based on the ideXlab platform.

  • effects of chronic sumatriptan and zolmitriptan treatment on 5 ht1 Receptor expression and function in rats
    Cephalalgia, 2004
    Co-Authors: Uwe Reuter, Salvatore Salomone, G W Ickenstein, Christian Waeber
    Abstract:

    Triptans are commonly used anti-migraine drugs and show agonist action mainly at serotonin 5-HT1B/1D/1F Receptors. It is not known whether frequent or long-term treatment with these drugs would alter 5-HT Receptor function. We investigated the effects of protracted (14-18 days) sumatriptan and zolmitriptan treatment in rats on 5-HT1 Receptor mRNA expression and function in tissues related to migraine pathophysiology. RT-PCR analysis revealed that 5-HT1B/1D/1F Receptor mRNA was reduced in the trigeminal ganglion after treatment with either triptan (reduction by: sumatriptan 39% and zolmitriptan 61% for 5-HT1B; 60% vs 41% for 5-HT1D; 32% vs 68% for 5-HT1F). Sumatriptan attenuated 5-HT1D Receptor mRNA by 49% in the basilar artery, whereas zolmitriptan reduced 5-HT1B mRNA in this tissue by 70%. No change in 5-HT1 Receptor mRNA expression was observed in coronary artery and dura mater. Chronic triptan treatment had no effect in two functional assays [sumatriptan mediated inhibition (50 mg/kg, i.p.) of electric...

José M. Palacios - One of the best experts on this subject based on the ideXlab platform.

  • Localization of 5-HT1B, 5-HT1Dα, 5-HT1E and 5-HT1F Receptor messenger RNA in rodent and primate brain
    Neuropharmacology, 1994
    Co-Authors: Anne T. Bruinvels, Bernhard Landwehrmeyer, Margaret M. Durkin, Daniel Hoyer, Guadalupe Mengod, Eric L Gustafson, Theresa Branchek, José M. Palacios
    Abstract:

    In situ hybridization histochemistry (ISHH) was used to study the distribution of various 5-HT1 Receptor messenger RNAs (mRNA) in the mammalian nervous system. Since the cDNAs encoding the different 5-HT1 Receptors, have not been cloned in one single species, brains of the species appropriate for the 5-HT1 Receptor messenger RNA (mRNA) have been used. Thus, 5-HT1B and 5-HT1Dα, mRNA were determined in rat and mouse brain, while 5-HT1E and 5-HT1F mRNA were studied in human (and monkey) and guinea-pig brain, respectively. 5-HT1B and 5-HT1Dα hybridization signals were predominantly present in caudate-putamen and cortical areas; in addition, 5-HT1B mRNA was also detected in hippocampus, cerebellum and cerebral arteries. In general, the distribution of 5-HT1B mRNA was characterized by high densities, whereas 5-HT1Dα mRNA was expressed at very low levels. Comparison of the localization of the mRNAs to the regional distributions of the 5-HT1B and 5-HT1D binding sites in rat brain (described in a previous study), revealed that both Receptor subtypes could be putative presynaptic heteroReceptors, modulating the release of various neurotransmitters in the central nervous system. The mRNA encoding the recently cloned 5-HT1E Receptor, which has low affinity for the 5-HT1 Receptor ligand 5-carboxamidotryptamine (5-CT), was localized in human brain. It was found to be present in cortical areas, caudate, putamen and amygdala, areas known to contain 5-CT insensitive 5-HT1 binding sites. The regional distribution of the 5-HT1Fip mRNA was determined in guinea-pig brain: high densities were observed in various cortical areas, the hippocampal formation and claustrum, which are regions known to contain 5-CT insensitive 5-HT1 or non 5-HT1A/1B/1C/1D[3H]5-HT binding sites. Altogether, this ISHH study describes the distribution of mRNAs of recently cloned 5-HT1 Receptors in rodent and primate brain and compares these results to the distribution of the heterogeneous population of 5-HT1 binding sites.

  • Localization of 5-HT1B, 5-HT1D alpha, 5-HT1E and 5-HT1F Receptor messenger RNA in rodent and primate brain.
    Neuropharmacology, 1994
    Co-Authors: Anne T. Bruinvels, Bernhard Landwehrmeyer, Margaret M. Durkin, Daniel Hoyer, Guadalupe Mengod, Eric L Gustafson, Theresa Branchek, José M. Palacios
    Abstract:

    In situ hybridization histochemistry (ISHH) was used to study the distribution of various 5-HT1 Receptor messenger RNAs (mRNA) in the mammalian nervous system. Since the cDNAs encoding the different 5-HT1 Receptors, have not been cloned in one single species, brains of the species appropriate for the 5-HT1 Receptor messenger RNA (mRNA) have been used. Thus, 5-HT1B and 5-HT1D alpha mRNA were determined in rat and mouse brain, while 5-HT1E and 5-HT1F mRNA were studied in human (and monkey) and guinea-pig brain, respectively. 5-HT1B and 5-HT1D alpha hybridization signals were predominantly present in caudate-putamen and cortical areas; in addition, 5-HT1B mRNA was also detected in hippocampus, cerebellum and cerebral arteries. In general, the distribution of 5-HT1B mRNA was characterized by high densities, whereas 5-HT1D alpha mRNA was expressed at very low levels. Comparison of the localization of the mRNAs to the regional distributions of the 5-HT1B and 5-HT1D binding sites in rat brain (described in a previous study), revealed that both Receptor subtypes could be putative presynaptic heteroReceptors, modulating the release of various neurotransmitters in the central nervous system. The mRNA encoding the recently cloned 5-HT1E Receptor, which has low affinity for the 5-HT1 Receptor ligand 5-carboxamidotryptamine (5-CT), was localized in human brain. It was found to be present in cortical areas, caudate, putamen and amygdala, areas known to contain 5-CT insensitive 5-HT1 binding sites. The regional distribution of the 5-HT1F mRNA was determined in guinea-pig brain: high densities were observed in various cortical areas, the hippocampal formation and claustrum, which are regions known to contain 5-CT insensitive 5-HT1 or non 5-HT1A/1B/IC/ID [3H]5-HT binding sites. Altogether, this ISHH study describes the distribution of mRNAs of recently cloned 5-HT1 Receptors in rodent and primate brain and compares these results to the distribution of the heterogeneous population of 5-HT1 binding sites.

Theresa Branchek - One of the best experts on this subject based on the ideXlab platform.

  • Localization of 5-HT1B, 5-HT1Dα, 5-HT1E and 5-HT1F Receptor messenger RNA in rodent and primate brain
    Neuropharmacology, 1994
    Co-Authors: Anne T. Bruinvels, Bernhard Landwehrmeyer, Margaret M. Durkin, Daniel Hoyer, Guadalupe Mengod, Eric L Gustafson, Theresa Branchek, José M. Palacios
    Abstract:

    In situ hybridization histochemistry (ISHH) was used to study the distribution of various 5-HT1 Receptor messenger RNAs (mRNA) in the mammalian nervous system. Since the cDNAs encoding the different 5-HT1 Receptors, have not been cloned in one single species, brains of the species appropriate for the 5-HT1 Receptor messenger RNA (mRNA) have been used. Thus, 5-HT1B and 5-HT1Dα, mRNA were determined in rat and mouse brain, while 5-HT1E and 5-HT1F mRNA were studied in human (and monkey) and guinea-pig brain, respectively. 5-HT1B and 5-HT1Dα hybridization signals were predominantly present in caudate-putamen and cortical areas; in addition, 5-HT1B mRNA was also detected in hippocampus, cerebellum and cerebral arteries. In general, the distribution of 5-HT1B mRNA was characterized by high densities, whereas 5-HT1Dα mRNA was expressed at very low levels. Comparison of the localization of the mRNAs to the regional distributions of the 5-HT1B and 5-HT1D binding sites in rat brain (described in a previous study), revealed that both Receptor subtypes could be putative presynaptic heteroReceptors, modulating the release of various neurotransmitters in the central nervous system. The mRNA encoding the recently cloned 5-HT1E Receptor, which has low affinity for the 5-HT1 Receptor ligand 5-carboxamidotryptamine (5-CT), was localized in human brain. It was found to be present in cortical areas, caudate, putamen and amygdala, areas known to contain 5-CT insensitive 5-HT1 binding sites. The regional distribution of the 5-HT1Fip mRNA was determined in guinea-pig brain: high densities were observed in various cortical areas, the hippocampal formation and claustrum, which are regions known to contain 5-CT insensitive 5-HT1 or non 5-HT1A/1B/1C/1D[3H]5-HT binding sites. Altogether, this ISHH study describes the distribution of mRNAs of recently cloned 5-HT1 Receptors in rodent and primate brain and compares these results to the distribution of the heterogeneous population of 5-HT1 binding sites.

  • Localization of 5-HT1B, 5-HT1D alpha, 5-HT1E and 5-HT1F Receptor messenger RNA in rodent and primate brain.
    Neuropharmacology, 1994
    Co-Authors: Anne T. Bruinvels, Bernhard Landwehrmeyer, Margaret M. Durkin, Daniel Hoyer, Guadalupe Mengod, Eric L Gustafson, Theresa Branchek, José M. Palacios
    Abstract:

    In situ hybridization histochemistry (ISHH) was used to study the distribution of various 5-HT1 Receptor messenger RNAs (mRNA) in the mammalian nervous system. Since the cDNAs encoding the different 5-HT1 Receptors, have not been cloned in one single species, brains of the species appropriate for the 5-HT1 Receptor messenger RNA (mRNA) have been used. Thus, 5-HT1B and 5-HT1D alpha mRNA were determined in rat and mouse brain, while 5-HT1E and 5-HT1F mRNA were studied in human (and monkey) and guinea-pig brain, respectively. 5-HT1B and 5-HT1D alpha hybridization signals were predominantly present in caudate-putamen and cortical areas; in addition, 5-HT1B mRNA was also detected in hippocampus, cerebellum and cerebral arteries. In general, the distribution of 5-HT1B mRNA was characterized by high densities, whereas 5-HT1D alpha mRNA was expressed at very low levels. Comparison of the localization of the mRNAs to the regional distributions of the 5-HT1B and 5-HT1D binding sites in rat brain (described in a previous study), revealed that both Receptor subtypes could be putative presynaptic heteroReceptors, modulating the release of various neurotransmitters in the central nervous system. The mRNA encoding the recently cloned 5-HT1E Receptor, which has low affinity for the 5-HT1 Receptor ligand 5-carboxamidotryptamine (5-CT), was localized in human brain. It was found to be present in cortical areas, caudate, putamen and amygdala, areas known to contain 5-CT insensitive 5-HT1 binding sites. The regional distribution of the 5-HT1F mRNA was determined in guinea-pig brain: high densities were observed in various cortical areas, the hippocampal formation and claustrum, which are regions known to contain 5-CT insensitive 5-HT1 or non 5-HT1A/1B/IC/ID [3H]5-HT binding sites. Altogether, this ISHH study describes the distribution of mRNAs of recently cloned 5-HT1 Receptors in rodent and primate brain and compares these results to the distribution of the heterogeneous population of 5-HT1 binding sites.

  • Molecular biology of the 5-HT1 Receptor subfamily
    Drug Development Research, 1992
    Co-Authors: Paul R. Hartig, Nika Adham, John M. Zgombick, Richard L. Weinshank, Theresa Branchek
    Abstract:

    Four serotonin Receptor clones have now been isolated and characterized. They encode the serotonin 5-HT1A, 5-HT1C, 5-HT1D, and 5-HT2 Receptors. The serotonin 5-HT1C Receptor, which was originally classified as a 5-HT1 Receptor, is now seen to be a member of the 5-HT2 Receptor subfamily. Within the current 5-HT1 Receptor subfamily, the two clones that have been described (5-HT1A and 5-HT1D) show similarities in amino acid sequence and function but are not as closely related as might have been expected. The human 5-HT1D Receptor clone, when expressed in mouse fibroblast cells, displays pharmacological binding properties in agreement with human cortical membrane preparations. Sumatriptan, a new antimigraine medication, exhibits an apparent dissociation constant of 3.4 nM at this human Receptor site. This represents the highest affinity interaction yet identified for this drug, and suggests that significant species differences may exist in the binding of this compound to 5-HT1D Receptors. Similar species differences in ergot drug affinities have been described for the 5-HT2 Receptor. Deduced amino acid sequence homologies between serotonin and other monoamine Receptor clones are discussed, leading to a classification scheme for serotonin Receptors involving superfamily, family, and subfamily relationships. © 1992 Wiley-Liss, Inc.

Peter J. Goadsby - One of the best experts on this subject based on the ideXlab platform.

  • Serotonin 5-HT1B/1D Receptor Agonists in Migraine
    CNS Drugs, 1998
    Co-Authors: Peter J. Goadsby
    Abstract:

    The development and clinical use of the serotonin 5-HT1 Receptor agonists, collectively known as the ‘triptans’, has ushered in a new age for clinicians treating patients with migraine, as well as a new era for those who respond to the medicines. The triptans that are currently in use (sumatriptan, naratriptan, rizatriptan and zolmitriptan) and those in development [almotriptan, eletriptan and frovatriptan (SB-209509, VML-251)] all share a common pharmacology of 5-HT1B/1D Receptor agonist activity.

Edith Hamel - One of the best experts on this subject based on the ideXlab platform.

  • effects of acute or chronic administration of anti migraine drugs sumatriptan and zolmitriptan on serotonin synthesis in the rat brain
    Cephalalgia, 2004
    Co-Authors: C Dobson, Y Tohyama, Mirko Diksic, Edith Hamel
    Abstract:

    Triptans are 5-HT1 Receptor agonists used as anti-migraine drugs. They act primarily on meningeal blood vessels and on trigeminovascular afferents, but they may also exert central effects. We studied the regional effects of acute and chronic treatment with sumatriptan or zolmitriptan on the rate of serotonin (5-HT) synthesis in the rat brain, using the α-14C-methyl-L-tryptophan quantitative autoradiographic method. Sumatriptan at low (300 μg/kg, s.c.) and high (1 mg/kg) doses, as well as zolmitriptan (100 μg/kg), acutely decreased (15-40%, P < 0.05-0.001) 5-HT synthetic rate in many brain regions, including the dorsal raphe nucleus. Chronically, sumatriptan (21 days, approximately 300 μg/kg per day via osmotic minipumps) induced significant increases in the 5-HT synthesis rate in many projection areas but had no effect in the dorsal raphe nucleus. The acute effects on 5-HT synthesis rate would be compatible with activation of 5-HT1 autoReceptors that inhibit serotonin release. In contrast, the increased 5...