Further evidence that vascular serotonin receptors are of the 5HT2 type

Cohen, Marlene L.; Mason, Norman R.; Wiley, Kathryn S.; Fuller, Ray W.

doi:10.1016/0006-2952(83)90541-5

Cited by 68 publications

(23 citation statements)

References 9 publications

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“…The 5-HT receptors mediating contraction of the rabbit aorta, the rat caudal artery and the rat jugular vein have been claimed to belong to the same class, namely the 5-HT2 type Humphrey et al, 1982;Cohen et al, 1983;Maayani et al, 1984). In this paper we have investigated the extent to which this classification can be sustained when these recep- tors, and the ligands which have been used to classify them, are analysed quantitatively using well-established pharmacological criteria (Schild, 1968;Black et al, 1983a).…”

Section: Discussionmentioning

confidence: 99%

“…Many antagonists, notably spiperone and ketanserin, have emerged from radioligand binding studies where they demonstrated high affinity for 5-HT2 binding sites in the brain (Peroutka & Snyder, 1979, 198 1;Leysen et al, 1982;Engel et al, 1984). The binding affinity of these and a range of other chemically diverse ligands appeared to correlate with their antagonist potencies measured in isolated tissues Van Nueten et al, 1982;Cohen et al, 1983;Miiller-Schweinitzer & Engel, 1983;Engel et al, 1984) leading to their widespread application as peripheral 5-HT2 receptor probes Feniuk et al, 1983a;Frenken & Kaumann, 1984;Cohen et al, 1985).…”

Section: Introductionmentioning

confidence: 99%

“…In an attempt to resolve this problem, we have conducted a between-tissues study of the 5-HT receptor antagonism obtained with the putative 5-HT2 antagonists ketanserin, spiperone, trazodone and methysergide. Experiments were performed in the rabbit aorta, the rat jugular vein and the rat caudal artery, each of which is claimed to contain 5-HT2 receptors on the basis of affinity correlations with the central 5-HT2 binding site Humphrey et al, 1982;Cohen et al, 1983;Maayani et al, 1984). Data were analysed strictly according to the established criteria for simple competition.…”

Section: Introductionmentioning

confidence: 99%

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Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?

Leff

Martin

1986

British J Pharmacology

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1 Interactions between 5-hydroxytryptamine (5-HT) and the so-called 5-HT2 receptor antagonists ketanserin, spiperone, trazodone and methysergide were studied in isolated preparations of the rabbit aorta, rat jugular vein, and rat caudal artery. 2 Trazodone and spiperone were apparently simple competitive antagonists since they produced antagonism that was surmountable over the concentration range studied and, in each tissue, their apparent affinity appeared to be independent of the antagonist concentration. Furthermore, concentration-ratios obtained with the two antagonists in combination suggested that antagonism was additive, implying mutual competition with a single population of 5-HT receptors. 3 Ketanserin was a non-surmountable antagonist of 5-HT in the rat caudal artery and methysergide demonstrated surmountable, competitive antagonism only in the rabbit aorta. 4 Antagonist dissociation constants estimated for apparently competitive interactions showed that ketanserin, spiperone and trazodone expressed affinities which differed according to the tissue used. In the case of trazodone, affinity estimates differed by as much as 12 fold. These discrepancies were independent of the 5-HT receptor agonist used and could not be attributed to an inadequate equilibration of the antagonist. 5These results can be interpreted in two ways: either the receptors in the different tissues are heterogeneous or the antagonists used here must be considered as unreliable probes for the classification of 5-HT2-like receptors.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?

Leff

Martin

1986

British J Pharmacology

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“…Furthermore, the hypertension produced by serotonin has been shown to be mediated through 5HT2-receptors in the peripheral blood vessels (5)(6)(7). Serotonin receptors have been demonstrated in the various tissues, and highly significant correlations were found between the concentration of the compound necessary for half-maximal contraction of vessels (ED50) and the binding affinity for binding sites (8).…”

Section: Discussionmentioning

confidence: 99%

Effects of bunitrolol on adrenergic and serotonergic receptors.

Tsuchihashi¹,

Aono²,

Nagatomo³

et al. 1987

Jpn.J.Pharmacol

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Abstract-To assess the importance of anti-adrenergic and anti-serotonergic activities of bunitrolol for its efficacy as an antihypertensive and antianginal agent, effects of this substance on the binding of adrenergic and serotonergic agents to the respective receptors of the rat brain, rat heart, dog brain, and/or dog aorta were examined using the radioligand binding assay methods.In addition, the pA2 values of bunitrolol as an antagonist against the positive chronotropic and inotropic actions (Q1-adrenoceptor) of isoproterenol were also determined by pharmacological methods using the isolated guinea pig atria. To assess the specificity, pA2 values were also obtained in the isolated trachea (132-adrenoceptor) using isoproterenol as an agonist and in the isolated aorta from the guinea pig and the rat using phenylephrine as an agonist (a,-adrenoceptor).

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“…Its potency for blocking 5-HT receptors is about 20 times less than its potency for blocking a-adrenoceptors. Since the receptors involved in the vascular response to 5-HT appear to be 5-HT2-receptors (Cohen et al, 1981;1983b) (Miller, 1967). Therefore, it is likely that the shifts in the concentration-response curve to carbachol reflect cholinoceptor antagonism rather than decreased myogenic tone.…”

Section: Vascular Smooth Muscle Relaxationmentioning

confidence: 99%

Pharmacological activity of ACC‐7513, a selective α‐adrenoceptor and 5‐hydroxytryptamine receptor blocking agent

Anderson¹,

Kam²

1985

British J Pharmacology

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I The pharmacological activity of N-[2-(2,6-dimethoxyphenoxy) ethyl]-2-(2-methoxyphenoxy) ethanaminium chloride (ACC-7513) was determined in isolated smooth and cardiac muscle and its effect on blood pressure and heart rate assessed in the spontaneously hypertensive rat (SHR). 2 ACC-7513 was found to be a potent a-adrenoceptor blocking agent (pA2: 8.33) and a 5-hydroxytryptamine (5-HT) antagonist (pA2:7.01), both in rabbit aortic strips. The affinity for aadrenoceptors was about 20 times greater than that for 5-HT-receptors.3 High concentrations of ACC-7513 did not block histamine in rabbit aortic strips, or 13,-or P2-adrenoceptor responses induced by isoprenaline in guinea-pig right atria and trachea, respectively, but did block cholinoceptor responses induced by carbachol in rat uterus, non-competitively. 4 High concentrations of ACC-7513 also produced sino-atrial depression in guinea-pig right atria and direct relaxation of depolarized rabbit aortic strips. 5 ACC-7513 depressed blood pressure of conscious SHRs and produced a reflex increase in heart rate. The reductions in pressure were modest and of short duration. 6 It is concluded that: (a) ACC-7513 is a potent, selective a-adrenoceptor and 5-HT receptor antagonist; and (b) ACC-7513 is not likely to be useful in the treatment of hypertension.

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Further evidence that vascular serotonin receptors are of the 5HT2 type

Cited by 68 publications

References 9 publications

Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?

Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?

Effects of bunitrolol on adrenergic and serotonergic receptors.

Pharmacological activity of ACC‐7513, a selective α‐adrenoceptor and 5‐hydroxytryptamine receptor blocking agent

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Further evidence that vascular serotonin receptors are of the 5HT2 type

Cited by 68 publications

References 9 publications

Peripheral 5‐HT2‐like receptors. Can they be classified with the available antagonists?

Peripheral 5‐HT2‐like receptors. Can they be classified with the available antagonists?

Effects of bunitrolol on adrenergic and serotonergic receptors.

Pharmacological activity of ACC‐7513, a selective α‐adrenoceptor and 5‐hydroxytryptamine receptor blocking agent

Contact Info

Product

Resources

About

Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?

Peripheral 5‐HT₂‐like receptors. Can they be classified with the available antagonists?