5‐HT<sub>1</sub>‐like receptors mediate 5‐hydroxytryptamine‐induced contraction of guinea‐pig isolated iliac artery

Şahin-Erdemli, İnci; Hoyer, Daniel; Stoll, A.; Seiler, Max P.; Schoeffter, Philippe

doi:10.1111/j.1476-5381.1991.tb12183.x

Cited by 47 publications

(26 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Membranes prepared from COS-7 cells transiently expressing the gene product bound [3H]LSD in a saturable and dose-dependent manner with an estimated Kd of 0.9 nM and a receptor, density of 0.8-1.2 pmol/mg of protein (Fig. 3a) (45)(46)(47). Furthermore, the finding that L17 is present in the Lymnaea heart suggests that this 5-HT receptor may be (41).…”

Section: Resultsmentioning

confidence: 99%

“…The localization of this receptor to defined neurons within the CNS of Lymnaea and further characterization may help to determine, for example, if it is involved in any behaviors such as learning and memory as described for Aplysia. The finding that 5HTlym is present in the Lymnaea heart and that vascular 5HT1-like 5-HT receptors (45)(46)(47) have been postulated to exist in mammals that appear not to be of a previously defined 5HT1 receptor type suggests that 5HTlym may belong to an additional subclass of 5HT1-like receptors common to mammals.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Sugamori

Sunahara

Guan

et al. 1993

Proc. Natl. Acad. Sci. U.S.A.

129

View full text Add to dashboard Cite

Serotonin (5-HT) is a major neurotransmitter that influences various behaviors, neuronal plasticity, learning, and memory in molluscs. Although the physiology of 5-HT transmission in molluscs is well studied, little is known about the pharmacology and diversity of the 5-HT receptor system. Based on the high homology of genes coding for guanine nucleotide-binding protein (G protein)-coupled receptors, we have cloned a gene for the Lymnaea stagnalis 5-HT (5HTlym) receptor. The putative receptor protein, 509 amino acids long, has highest homology with the Drosophila 5-HT receptors and mammalian 5HT1 receptors. As revealed by RNA blot-hybridization analysis, two mRNA species of 2.3 and 3.2 kb are detected in the central nervous system of Lymnaea. Transient expression of 5HTlym in COS-7 cells showed saturable [3H]lyseric acid diethylamide binding with an estimated dissociation constant of 0.9 nM. The 5HTlym receptor exhibited a mixed 5HT-like pharmacology that cannot be precisely categorized with existing mammalian classification nomenclature. However, the 5HTlym receptor does display some characteristics that have been attributed to the putative mammalian vascular 5HT1-like receptor.Serotonin (5-HT), a neurotransmitter that mediates a number of effects through several different receptors, is present in both vertebrate and invertebrate species (1, 2). In mammals several 5-HT receptors and receptor subtypes have been identified based on pharmacological and biochemical criteria (3)(4)(5)(6). Presently, seven distinct mammalian 5-HT receptors have been cloned. These include the SHT1A (7,8), SHT1B (9), 5HT1c (10, 11), 5HT1Da (12), 5HT1Dp (13,14), SHT2 (11,15,16), and the pharmacologically uncharacterized human 5-HT receptor, S31 (17), all of which mediate their effects through coupling to guanine nucleotide-binding regulatory proteins (G proteins). In addition, three 5-HT receptors in Drosophila melanogaster-the 5HTdro1 receptor (18), which stimulates adenylate cyclase, and the 5HTdro2A and 5HTdro2B receptors (19), which inhibit adenylate cyclase-have recently been cloned. These receptors in Drosophila are most homologous in primary sequence to the human SHT1A receptor; however, the partial pharmacological characterization of these receptors suggests that they are not identical to the 5HT1A receptor.The molluscan nervous system contains large amounts of 5-HT, and several 5-HT-containing neurons have been identified therein (20,21). The effect of 5-HT on various ionic currents and on the cell membrane potential has been studied extensively in molluscs, and on the basis of these experiments the existence of several 5-HT receptors has been postulated (22, 23). 5-HT also has been implicated in many behavioral or physiological processes in molluscs such as learning, circadian rhythms, feeding, development, and neuronal regeneration (24-32). The 5-HT receptors that mediate the behavioral and/or electrophysiological effects are structurally and pharmacologically not well characterized, and none of these receptors has be...

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Sugamori

Sunahara

Guan

et al. 1993

Proc. Natl. Acad. Sci. U.S.A.

129

View full text Add to dashboard Cite

show abstract

“…For example, in guinea pig isolated iliac arteries 5-HT 1 -like silent receptor appears only in the presence of vascular tone. 20) The same phenomenon has been described in bovine isolated pulmonary arteries 21) and in rabbit isolated mesenteric arteries, 22) where preconstriction of the tissue with different contractile agents revealed potent vasoconstrictory effects of 5-HT. In rat aorta, a mutual amplification in contractile responses by simultaneous activation of a 1 and 5-HT 2 receptors has been described.…”

mentioning

confidence: 62%

“…The descending aorta was carefully removed, cleaned, and cut into 3 or 4 rings 4 mm in length which were then mounted in organ baths containing 20 When required, the endothelium was removed mechanically by rotating the vessel along a cotton bud. All the tissues were allowed to stabilize for 60 min under 2 g of resting tension, with washing every 15 min.…”

Section: Methodsmentioning

confidence: 99%

Functional Characterization of Serotonin Receptors in Rat Isolated Aorta.

Villazón¹,

Padín²,

Cadavid³

et al. 2002

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

The complex actions of serotonin (5-HT) on blood vessels is attributed to interactions with a multiplicity of specific 5-HT receptors located in smooth muscle and endothelium, sometimes mediating opposite effects.In the case of rat aorta, at least the 5-HT 2A receptor is functionally present 1) and it mediates potent vasoconstriction with a relatively low affinity for 5-HT. Apart from this receptor, 5-HT 2B , 5-HT 1B , and 5-HT 7 mRNAs have been detected in this tissue 2) by polymerase chain reaction (PCR) techniques. The corresponding receptors mediate different responses in the isolated preparations where they have been functionally described: the 5-HT 2B receptor has been located in the endothelium of pig pulmonary artery 3,4) and rat jugular vein, 5) mediating relaxation. It has also been proposed that this receptor in smooth muscle mediates vasoconstriction in the mesenteric artery of mineralocorticoid hypertensive rats.6,7) The 5-HT 1B receptor has been described in a variety of tissues (for example, human coronary arteries, 8) rabbit epicardial coronary arteries, 9) human temporal artery, 10) human and bovine cerebral arteries 11) ) and mediates vasoconstriction when located in smooth muscle or relaxation when in endothelium. The 5-HT 7 receptor is located in smooth muscle, where it induces vasorelaxation (for a review see 12) ) in many preparations such as canine coronary and cerebral arteries, 13,14) dog basilar artery and cerebral blood vessels, 15,16) and cynomolgus monkey isolated jugular vein. 17)In addition, functional effects of some of these receptors appear to be related to the preconstriction of the tissue. Thus contractile synergism between 5-HT and other vasoconstrictor substances has been observed in peripheral and cerebrovascular blood vessels (for a review see 18,19) ). For example, in guinea pig isolated iliac arteries 5-HT 1 -like silent receptor appears only in the presence of vascular tone.20) The same phenomenon has been described in bovine isolated pulmonary arteries 21) and in rabbit isolated mesenteric arteries, 22) where preconstriction of the tissue with different contractile agents revealed potent vasoconstrictory effects of 5-HT. In rat aorta, a mutual amplification in contractile responses by simultaneous activation of a 1 and 5-HT 2 receptors has been described. 23) This phenomenon may play an important role in certain pathological states such as hypertension, peripheral vascular disease, and coronary spasm.18) The importance of preconstriction is even greater in the case of relaxant receptors because normally preconstriction is needed for a relaxant response to occur.Taking all these data together, the effects of 5-HT on blood vessels are complex and dependent on the anatomical location of the receptors and on additional factors such as preconstriction of the tissue with a non-5-HT receptor agonist that could unmask previously inactive or "silent" 5-HT receptor subtypes. In the preparation we have studied, rat aorta, the presence of mRNA for different 5-HT receptors (5-HT 2B...

show abstract

“…The range of 5-HT receptor antagonists shown in Table which (Connell & Wallis, 1989;Larkman & Kelly, 1991) or the dopaminergic neurones of the guinea-pig substantia nigra (Nedergaard et al, 1991), but the lack of action of sumatriptan would rule out some vascular tissue receptors (e.g. Sahin-Erdemli et al, 1991). From the data in Table 1 (Knoper et al, 1992;Matsumoto et al, 1993).…”

Section: Discussionmentioning

confidence: 99%

Multiple 5‐HT receptors in the guinea‐pig superior cervical ganglion

Watkins

Newberry

1996

British J Pharmacology

View full text Add to dashboard Cite

1 We have studied the pharmacology of the depolarization by 5-hydroxytryptamine (5-HT) of the guinea-pig isolated superior cervical ganglion (SCG) using the grease-gap technique. We studied the effects of selective and non-selective antagonists on the responses to 5-HT and other 5-HT receptor agonists. 2 We have extended the pharmacology of the 5-HT3 receptor in this preparation by studying the effects of granisetron, BRL 46470 and mianserin on the concentration-response curve (CRC) to 2-methyl-5-HT. As with other 5-HT3 receptor antagonists, these compounds exhibited a lower affinity for guinea-pig 5-HT3 receptors than for rat 5-HT3 receptors. 3 We have confirmed that low concentrations of 5-HT (< 1 uM) mediate ketanserin-sensitive responses and higher concentrations of 5-HT also recruit 5-HT3 receptors. The responses to low concentrations of 5-HT were antagonized by, low concentrations of ketanserin, spiperone, mianserin, DOI and LSD indicating probably mediation by 5-HT2A receptors. At high concentrations, the hallucinogen, DOI, but not LSD, evoked a ketanserin-sensitive depolarization. 4 Although mianserin could bind to the 5-HT2A receptors in this preparation, we could not demonstrate a down-regulation of depolarizations evoked by these receptors after a 10 day oral treatment with mianserin (10 mg kg-', daily). 5 5-Carboxamidotryptamine (5-CT) evoked a prolonged depolarization. Although high concentrations of 5-CT (> 1 ,uM) appeared to activate 5-HT2A receptors, lower concentrations of 5-CT evoked a response with a distinct pharmacology. After studying the action of 20 selective and non-selective 5-HT receptor ligands we believe that this response may be mediated by a novel receptor; but its pharmacology is closest to that of receptors in the 5-HT2 receptor family. Like 5-CT, 5-HT (3 -300 ,uM) could evoke an LSD-sensitive response in the presence of the 5-HT2 receptor antagonist, ketanserin and the 5-HT3 receptor antagonist, tropisetron (all 1 gM). 6 We conclude that 5-HT activates three pharmacologically distinct receptors to depolarize the guineapig SCG. Low concentrations of 5-HT appear to activate 5-HT2A receptors. Higher concentrations of 5-HT also activate 5-HT3 receptors and a possible novel 5-HT receptor. The novel receptor could be a species homologue of a 5-HT2 receptor or an, as yet, unclassified 5-HT receptor.

show abstract

5‐HT₁‐like receptors mediate 5‐hydroxytryptamine‐induced contraction of guinea‐pig isolated iliac artery

Cited by 47 publications

References 26 publications

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Functional Characterization of Serotonin Receptors in Rat Isolated Aorta.

Multiple 5‐HT receptors in the guinea‐pig superior cervical ganglion

Contact Info

Product

Resources

About

5‐HT1‐like receptors mediate 5‐hydroxytryptamine‐induced contraction of guinea‐pig isolated iliac artery

Cited by 47 publications

References 26 publications

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Serotonin receptor cDNA cloned from Lymnaea stagnalis.

Functional Characterization of Serotonin Receptors in Rat Isolated Aorta.

Multiple 5‐HT receptors in the guinea‐pig superior cervical ganglion

Contact Info

Product

Resources

About

5‐HT₁‐like receptors mediate 5‐hydroxytryptamine‐induced contraction of guinea‐pig isolated iliac artery