Effects of chlorprothixene isomers on platelet 5-hydroxytryptamine receptors: Evidence for different 5-hydroxytryptamine conformations at uptake and stimultory sites

Drummond, Alan H.; Whigham, Kathryn A. E.; Prentice, C. R. M.

doi:10.1016/0014-2999(76)90047-9

Cited by 4 publications

(3 citation statements)

References 8 publications

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“…those known to be tryptamine receptor agonists in other tissues, induced a shape change which was inhibited by methysergide. In addition, the receptor exhibited marked stereoselectivity for (+ -LSD and (+ )-butaclamol and, as described earlier, for cischlorprothixene (Drummond, Whigham & Prentice, 1976). Several of the compounds in Table 1 ((+)-LSD, psilocine, N',N'-dimethylated tryptamines) may be considered as mixed agonists-antagonists.…”

Section: Discussionmentioning

confidence: 98%

Shape Change of Blood Platelets—a Model for Cerebral 5‐hydroxytryptamine Receptors?

Gräf

Pletscher

1979

British J Pharmacology

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In blood platelets of rabbits isolated by a stractan gradient and incubated in a protein‐poor medium, tryptamine, 5‐hydroxytryptamine (5‐HT) and derivatives, quipazine and mescaline caused a shape change. This shape change was inhibited by low concentrations of methysergide. The most potent antagonists of the 5‐HT‐induced shape change included ergoline derivatives and neuroleptic drugs, which showed high stereoselectivity. (‐f)‐Lysergic acid diethylamide ((+)‐LSD), psilocine and some N',N′‐dimethylated tryptamines acted as mixed agonist‐antagonists. The compounds found to be agonists or mixed agonist‐antagonists on platelets have previously been shown to act also as 5‐HT agonists in the central nervous system (CNS). With regard to 5‐HT antagonists, the 5‐HT receptors of platelets reacted differently from those described earlier in brain areas with dense 5‐hydroxytryptaminergic innervation, but showed similarities to 5‐HT receptors investigated previously in spinal cord, cerebral cortex and possibly reticular formation. It is concluded that platelets may be considered with caution as models for some, but not for all, 5‐HT receptors in the CNS.

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Section: Discussionmentioning

confidence: 98%

Shape Change of Blood Platelets—a Model for Cerebral 5‐hydroxytryptamine Receptors?

Gräf

Pletscher

1979

British J Pharmacology

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“…However, the association between another group of antipsychotics-selective serotonin reuptake inhibitors and upper gastrointestinal bleeding was described by de Abajo et al (27) and Nelva et al (17) more than 20 years ago. The inhibition of the aggregation of human blood platelets caused by the administration of chlorprothixene was also observed and studied (28).…”

Section: Discussionmentioning

confidence: 99%

“… more than 20 years ago. The inhibition of the aggregation of human blood platelets caused by the administration of chlorprothixene was also observed and studied .…”

Section: Discussionmentioning

confidence: 99%

Black Esophagus: Acute Esophageal Necrosis in Fatal Haloperidol Intoxication

Hejna

Ublová

Voříšek

2013

Journal of Forensic Sciences

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Herein, we present a case of 53-year-old psychotic woman with acute esophageal necrosis (black esophagus), who was found lying on the floor in the living room of her flat. Pillboxes of antipsychotic drugs were located in the bin. External examination of the body was unremarkable. On internal examination, we found acute esophageal necrosis. Histologically, there was complete epithelial necrosis with focal involvement of muscularis mucosae, dense infiltrate of leukocytes, and ulcerations without any viable cells. There was no evidence of underlying organic diseases or trauma. Toxicological analysis revealed a fatal blood level of antipsychotics (haloperidol, zotepine, and chlorprothixene). Death of the deceased was attributed to fatal intoxication with three various types of antipsychotics. As far we know, this is the first described association between so-called black esophagus and fatal blood level of neuroleptics.

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Basic Pharmacological Properties

Müller‐Schweinitzer¹,

Weidmann²

1978

Ergot Alkaloids and Related Compounds

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Effects of chlorprothixene isomers on platelet 5-hydroxytryptamine receptors: Evidence for different 5-hydroxytryptamine conformations at uptake and stimultory sites

Cited by 4 publications

References 8 publications

Shape Change of Blood Platelets—a Model for Cerebral 5‐hydroxytryptamine Receptors?

Shape Change of Blood Platelets—a Model for Cerebral 5‐hydroxytryptamine Receptors?

Black Esophagus: Acute Esophageal Necrosis in Fatal Haloperidol Intoxication

Basic Pharmacological Properties

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