ChemInform Abstract: 1‐(INDOLYLMETHYL)‐1,2,3,4‐TETRAHYDROISOQUINOLINES AND 1‐BENZYL‐2,3,4,9‐TETRAHYDRO(1H)β‐CARBOLINES PREPARED FROM TRYPTAMINE OR FROM ITS DERIVATIVES

Gaignault, J.-C.; Fréchet, Denise; Nédélec, L.

doi:10.1002/chin.197921252

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1996

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“…The "partial yohimbines" 2, 25 34 and 32 35 are known compounds whose syntheses have been reported previously. Novel tetrahydro-β-carbolines (18-20, 23-25, 27-31, and 33-84) were prepared from their parent tryptamines and suitable carbonyl precursors by two methods.…”

Section: Chemistrymentioning

confidence: 99%

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus

et al. 1996

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A series of potent, selective 5HT2B receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT2B receptor affinity relative to the starting structure (-log KBS > 10.0 have been obtained). These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT2A and 5HT2C receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT2B receptor in normal and disease physiology.

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Section: Chemistrymentioning

confidence: 99%

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus

et al. 1996

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ChemInform Abstract: 1‐(INDOLYLMETHYL)‐1,2,3,4‐TETRAHYDROISOQUINOLINES AND 1‐BENZYL‐2,3,4,9‐TETRAHYDRO(1H)β‐CARBOLINES PREPARED FROM TRYPTAMINE OR FROM ITS DERIVATIVES

Abstract: Die Umsetzung des Dopamins (I) mit der Indolylessigsäure (II) liefert das Amid (III), das nach Cyclisierung mit Phosphoroxychlorid durch Natriumboranat zum Amin (IV) reduziert wird.

Cited by 1 publication

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Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus

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ChemInform Abstract: 1‐(INDOLYLMETHYL)‐1,2,3,4‐TETRAHYDROISOQUINOLINES AND 1‐BENZYL‐2,3,4,9‐TETRAHYDRO(1H)β‐CARBOLINES PREPARED FROM TRYPTAMINE OR FROM ITS DERIVATIVES

Abstract: Die Umsetzung des Dopamins (I) mit der Indolylessigsäure (II) liefert das Amid (III), das nach Cyclisierung mit Phosphoroxychlorid durch Natriumboranat zum Amin (IV) reduziert wird.

Cited by 1 publication

References 0 publications

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT2B) Contractile Receptor in the Rat Stomach Fundus

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT2B) Contractile Receptor in the Rat Stomach Fundus

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Product

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Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus

Potent, Selective Tetrahydro-β-carboline Antagonists of the Serotonin 2B (5HT_2B) Contractile Receptor in the Rat Stomach Fundus