Distinct 5-HT1B and 5-HT1D serotonin receptors in rat: Structural and pharmacological comparison of the two cloned receptors

Hamblin, Mark W.; McGuffin, Robert W.; Metcalf, Mark A.; Dorsa, Daniel M.; Merchant, Kalpana

doi:10.1016/1044-7431(92)90070-i

Cited by 105 publications

(71 citation statements)

References 33 publications

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“…However, both 5-HTlB and 5-HTlD recognition sites are present in rat brain (Herrick-Davis & Titeler, 1988;Bruinvels et al, 1992) and distinct 5-HT1B and 5-HT1D receptor genes have been identified (Hamblin et al, 1992). In man, two genes encode two receptors with 5-HTID pharmacology (Hamblin et al, 1992;see Hoyer et al, 1994), which Weinshank et al (1992) have termed 5-HTm. and 5-HTID,.…”

Section: Discussionmentioning

confidence: 99%

“…Further, the pKD of 6.2 for sumatriptan and the reported lack of agonist activity of sumatriptan at 5-ht7 receptors at 10 pM (Hoyer et al, 1994) 5-HT1B and 5-HTID receptors represented species variants controlled by a single gene, 5-HTlB receptors being expressed in rodents and 5-HTID receptors in other species (Hoyer & Middlemiss, 1989). However, both 5-HTlB and 5-HTlD recognition sites are present in rat brain (Herrick-Davis & Titeler, 1988;Bruinvels et al, 1992) and distinct 5-HT1B and 5-HT1D receptor genes have been identified (Hamblin et al, 1992). In man, two genes encode two receptors with 5-HTID pharmacology (Hamblin et al, 1992;see Hoyer et al, 1994), which Weinshank et al (1992) have termed 5-HTm.…”

Section: Discussionmentioning

confidence: 99%

“…The observed high affinity of sumatriptan ruled out many of these. Sumatriptan has a high affinity for 5-HTID and 5-HTIB receptors (Hoyer et al, 1994) with a pKi at rat 5-HTID and 5-HT1B receptors expressed in COS-7 cells of 8.0 and 7.35, respectively (Hamblin et al, 1992); at 5-htlF receptors the pKi is 7.2 (Boess & Martin, 1994). Crick et al (1994) estimated a pKA of 7.9 for sumatriptan as a depressant of the MSR in rat spinal cord (cf.…”

Section: Discussionmentioning

confidence: 99%

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Ketanserin‐sensitive depressant actions of 5‐HT receptor agonists in the neonatal rat spinal cord

Manuel¹,

Wallis²,

Crick³

1995

British J Pharmacology

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1 The monosynaptic reflex (MSR), recorded in vitro from the neonatal rat spinal cord, was depressed by 5-hydroxytryptamine (5-HT), 5-carboxamidotryptamine (5-CT), methysergide and R( + )-8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), and also by the selective 5-HTlD agonists, sumatriptan and N-methyl-3-(1-methyl-1-piperidinyl)-1H-indole-5-ethane sulphonamide (GR 85548).2 Ketanserin (1 gM) and methiothepin (1 gM) reduced the duration of depressions elicited by 5-CT, but not those produced by 5-HT, sumatriptan, GR 85548, methysergide or 8-OH-DPAT.3 The IC50 for MSR depression by 5-CT was 3.6, 2.1 -6.2nM (n=4), by sumatriptan was 15.2, 12.9-18.0nM (n=32), by GR 85548 was 18.4, 11.7-29.1 nM (n =12), by methysergide was 29.8, 10.2-87.1nM (n=4) and by 8-OH-DPAT was 0.21, 0.11-0.43 MM (n=3) (geometric means and 95% confidence limits). 4 Ketanserin (0.1 or 1 UM) antagonized competitively responses to sumatriptan (apparent pA2 7.8 ± 0.1, n = 5), GR 85548 (apparent pA2 7.6, unpaired data, n = 5), methysergide (apparent pA2 7.9 ± 0.12, n=4) and 8-OH-DPAT (apparent pA2 8.3 ± 0.1, n= 3). Concentration-response curves to 5-CT showed a smaller, parallel shift to the right (apparent pA2 6.8 ± 0.1, n = 4), but responses to 5-HT were unaffected by ketanserin (1 gM) (n = 4). Neither with these concentrations nor with concentrations in the range 1-3 nm was there any unequivocal blockade of responses to sumatriptan. 9 It is concluded that sumatriptan, GR 85548, methysergide and 8-OH-DPAT depress the MSR in the neonate rat spinal cord via ketanserin-sensitive receptors, which have some similarities to 5-HTLIT1 receptors but which are not blocked by GR 127935. 5-HT released by tryptaminergic pathways may act via the same receptors to depress the MSR. 5-HT applied to the cord probably acts via a different, possibly novel 5-HT receptor to depress the MSR.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Ketanserin‐sensitive depressant actions of 5‐HT receptor agonists in the neonatal rat spinal cord

Manuel¹,

Wallis²,

Crick³

1995

British J Pharmacology

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“…5-HT 1A mRNA was detected with an oligonucleotide probe corresponding to residues 1110-1151 [8]. For the 5-HT 1B probes, three oligonucleotides corresponding to residues 1343-1382, 1630-1668, and 1790-1829 of the rat 5-HT 1B clone, MG11B [19], were synthesized as previously described [31]. The probes were individually labeled with [ 33 P]-dATP (Andotek, Irvine, CA) using terminal deoxyribonucleotidyl transferase (Gibco, Gaithersburg, MD) and purified on NENSORB columns (Dupont NEN Research Products, Boston, MA).…”

Section: In Situ Hybridization Histochemistrymentioning

confidence: 99%

Corticosteroids regulate 5-HT1A but not 5-HT1B receptor mRNA in rat hippocampus

Neumaier

Sexton

Hamblin

et al. 2000

Molecular Brain Research

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The role of mineralocorticoid and glucocorticoid receptors (MR and GR, respectively) in the regulation of serotonin receptors has not been clearly delineated. There is no consensus regarding the regulation of 5-HT 1A receptors, and corticosteroid regulation of 5-HT 1B mRNA has not been previously studied. We compared the effects of long-term (two week) adrenalectomy (no MR or GR activation) and several hormone replacement protocols designed to stimulate MR selectively (ALDO), MR and GR (HCT), and continuous MR with cyclical GR activation (SHAM adrenalectomy). 5-HT 1A and 5-HT 1B mRNAs were measured by in situ hybridization in hippocampus and raphe nuclei. None of the experimental manipulations altered 5-HT 1B mRNA levels in the hippocampus or dorsal raphe, and also had no effect on 5-HT 1A mRNA in dorsal or median raphe. However, 5-HT 1A mRNA levels were regulated in a complex manner in the different subfields of hippocampus. We conclude that both MR and GR play an integrated role in regulating 5-HT 1A mRNA levels in hippocampus while having no effect on 5-HT 1B mRNA levels under these conditions.

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“…However, recent molecular cloning data indicates that at least six subtypes of 5-HTI receptors, 5-HTIA-IF, can now be differentiated in the CNS (Albert et al 1990;Julius et al 1988;Hamblin et al 1992;Lovenberg et al 1993;Adham et al 1993). Of these, the 5-HTIA recep tor is found in particularly high abundance within the hippocampus (Chalmers and Watson 1991;Pompeino et al 1992).…”

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confidence: 99%

Regulation of Hippocampal 5-HT1A Receptor Gene Expression by Dexamethasone

Chalmers

López

Vázquez

et al. 1994

Neuropsychopharmacol

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The effect of dexamethasone, a selective GR agonist, on hippocampal, 5-HT1A receptor mRNA expression and 5-HT1A binding was examined using in situ hybridization histochemistry and in vitro receptor autoradiography. One week after adrenalectomy, both 5-HT1A receptor mRNA expression and 5-HT1A binding were increased throughout the hippocampus. Administration of dexamethasone at the time of adrenalectomy significantly attenuated the increases in 5-HT1A mRNA expression in all hippocampal subfields (p < . OS, Fisher Test), although 5-HT1A mRNA levels

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Distinct 5-HT1B and 5-HT1D serotonin receptors in rat: Structural and pharmacological comparison of the two cloned receptors

Cited by 105 publications

References 33 publications

Ketanserin‐sensitive depressant actions of 5‐HT receptor agonists in the neonatal rat spinal cord

Ketanserin‐sensitive depressant actions of 5‐HT receptor agonists in the neonatal rat spinal cord

Corticosteroids regulate 5-HT1A but not 5-HT1B receptor mRNA in rat hippocampus

Regulation of Hippocampal 5-HT1A Receptor Gene Expression by Dexamethasone

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