The neuropharmacology of emesis: the role of receptors in neuromodulation of nausea and vomiting

1990 ◽  
Vol 68 (2) ◽  
pp. 279-288 ◽  
Author(s):  
R. A. Leslie ◽  
Y. Shah ◽  
M. Thejomayen ◽  
K. M. Murphy ◽  
H. A. Robertson
Keyword(s):  
Binding Sites ◽  
Nausea And Vomiting ◽  
Dopamine Antagonists ◽  
Dorsal Vagal Complex ◽  
Neurotransmitter Receptor ◽  
Receptor Sites ◽  
Muscarinic Binding Sites ◽  
The Central Nervous System ◽  
Muscarinic Cholinergic

The basic pharmacological mechanisms involved in mediating nausea and vomiting are still poorly understood. Several classes of drags have been identified that alleviate the symptoms of nausea and vomiting, either prophylactically or acutely. None of these is completely effective in all cases. They include antihistamines, dopamine antagonists, steroids, cannabinoids, benzodiazepines, serotonin antagonists, and anticholinergics. This paper examines the evidence that links each of these classes of drugs with the distribution of specific neurotransmitter receptor sites on which they may be acting. Studies on the central nervous system distribution of binding sites for one of these classes of drugs, the anticholinergics, are described. Binding sites for the muscarinic cholinergic radioligand [3H]quinuclidinyibenzilate occur in different concentrations throughout the dorsal vagal complex of the rabbit medulla oblongata. The distribution of such sites in this nonvomiting experimental animal is markedly different from that in the cat, an animal that has been used for many physiological and pharmacological studies of emesis. A previous study has suggested that muscarinic binding sites may occur presynaptically on vagal afferent terminals that synapse in the dorsal vagal complex of the cat; this appears not to be the case in the rabbit. Possible implications of these findings for the identification of the site of action of anticholinergic, antiemetic drags are discussed.Key words: neuromodulation, nausea, vomiting, receptors.

scholarly journals Adenosine Receptor Heteromers and their Integrative Role in Striatal Function

2007 ◽  
Vol 7 ◽  
pp. 74-85 ◽  
Author(s):  
Sergi Ferré ◽  
Francisco Ciruela ◽  
César Quiroz ◽  
Rafael Luján ◽  
Patrizia Popoli ◽  
...  
Keyword(s):  
Adenosine Receptor ◽  
Neurotransmitter Receptors ◽  
Neurotransmitter Receptor ◽  
Binding Characteristics ◽  
New Concepts ◽  
Receptor Heteromers ◽  
The Central Nervous System ◽  
The Individual ◽  
Striatal Function

By analyzing the functional role of adenosine receptor heteromers, we review a series of new concepts that should modify our classical views of neurotransmission in the central nervous system (CNS). Neurotransmitter receptors cannot be considered as single functional units anymore. Heteromerization of neurotransmitter receptors confers functional entities that possess different biochemical characteristics with respect to the individual components of the heteromer. Some of these characteristics can be used as a “biochemical fingerprint” to identify neurotransmitter receptor heteromers in the CNS. This is exemplified by changes in binding characteristics that are dependent on coactivation of the receptor units of different adenosine receptor heteromers. Neurotransmitter receptor heteromers can act as “processors” of computations that modulate cell signaling, sometimes critically involved in the control of pre- and postsynaptic neurotransmission. For instance, the adenosine A1-A2Areceptor heteromer acts as a concentration-dependent switch that controls striatal glutamatergic neurotransmission. Neurotransmitter receptor heteromers play a particularly important integrative role in the “local module” (the minimal portion of one or more neurons and/or one or more glial cells that operates as an independent integrative unit), where they act as processors mediating computations that convey information from diverse volume-transmitted signals. For instance, the adenosine A2A-dopamine D2receptor heteromers work as integrators of two different neurotransmitters in the striatal spine module.

Results of Antiemetic Management in Terminal Illness

1993 ◽  
Vol 9 (2) ◽  
pp. 19-21 ◽  
Author(s):  
Ivan Lichter
Keyword(s):  
Receptor Antagonist ◽  
Terminal Illness ◽  
Nausea And Vomiting ◽  
Neurotransmitter Receptor ◽  
Receptor Sites

A wide variety of causes may be responsible for nausea and vomiting in terminal illness. The different emetic stimuli reach the vomiting centre by a variety of pathways and can be blocked by specific antiemetics that act at the neurotransmitter receptor sites in these pathways. A knowledge of the neurotransmitter receptor antagonist potency of the different antiemetics allows the choice of the most appropriate antiemetic for the relief of the nausea and vomiting caused by a particular emetic stimulus. To demonstrate the efficacy of this approach to the management of nausea and vomiting in terminal illness, the outcome of antiemetic choice in 100 consecutive episodes is recorded.

Alpha- and beta-adrenergic and muscarinic cholinergic binding sites in the bladder and urethra of the rabbit

1983 ◽  
Vol 61 (1) ◽  
pp. 61-66 ◽  
Author(s):  
Anthony Johns
Keyword(s):  
Binding Site ◽  
Dissociation Constant ◽  
Receptor Binding ◽  
Binding Sites ◽  
Binding Assays ◽  
Muscarinic Binding Sites ◽  
Rabbit Urethra ◽  
Radioligand Receptor Binding ◽  
Muscarinic Cholinergic ◽  
Quinuclidinyl Benzilate

The affinities of a number of α and β-adrenergic binding sites and muscarinic cholinergic binding sites in rabbit urethra and bladder have been determined, using specific radioligand receptor binding assays. There was a greater density of β-binding sites than α-binding sites in the bladder, while, in the urethra, there was a greater density of α-binding sites than β-binding sites. The number of α-binding sites was fourfold greater in the urethra, whereas there were fewer β-binding sites in the urethra. There were fewer muscarinic binding sites in the urethra than in the bladder. The dissociation constant for [3H]dihydroalprenolol at the β-binding site was 6.4 nM, for [3H]dihydroergocryptine at the α-binding site was 2.11 nM, and for 3H-labelled l-quinuclidinyl benzilate at the muscarinic binding site was 0.22 nM.

Role of area postrema pressor mechanisms in the regulation of arterial pressure

1987 ◽  
Vol 65 (8) ◽  
pp. 1591-1597 ◽  
Author(s):  
Carlos M. Ferrario ◽  
Karen L. Barnes ◽  
Debra I. Diz ◽  
Christine H. Block ◽  
David B. Averill
Keyword(s):  
Angiotensin Ii ◽  
Binding Sites ◽  
Area Postrema ◽  
Intrinsic Activity ◽  
Motor Nucleus ◽  
Additional Information ◽  
The Central Nervous System ◽  
Nuclear Regions

This article discusses the data which established that angiotensin II modulates the tonic and reflex control of cardiovascular function by actions on the nuclear regions of the dorsal medulla oblongata. Although physiological evidence for the modulatory actions of angiotensin II in structures of the lower brainstem has been gathered over the past 16 years, only the recent application of new neurobiological techniques has allowed a more definitive understanding of its role. The identification of high affinity angiotensin II binding sites within the parenchyma of the area postrema with the technique of in vitro receptor autoradiography has provided anatomical validity for a role of angiotensin II in the central nervous system. The added discovery of angiotensin II binding sites in subnuclear components of the nucleus tractus solitarii and the motor nucleus of the tenth cranial nerve provides additional information on the various mechanisms through which angiotensin II may affect the intrinsic activity of the brainstem neuronal circuits involved in the integration of baroreceptor and sensory visceromotor function.

Interaction of antipsychotic drugs with neurotransmitter receptor sites in vitro and in vivo in relation to pharmacological and clinical effects: role of 5HT2 receptors

1993 ◽  
Vol 112 (S1) ◽  
pp. S40-S54 ◽  
Author(s):  
Josée E. Leysen ◽  
Paul M. F. Janssen ◽  
Alain Schotte ◽  
Walter H. M. L. Luyten ◽  
Anton A. H. P. Megens
Keyword(s):  
Antipsychotic Drugs ◽  
Clinical Effects ◽  
Neurotransmitter Receptor ◽  
Receptor Sites ◽  
5Ht2 Receptors

Juvenile xanthogranuloma of the subdural spaces mimicking chronic hematoma with positive FDG uptake on PET: case report

2020 ◽  
Vol 26 (4) ◽  
pp. 449-453
Author(s):  
Jacob A. Kahn ◽  
Jeffrey T. Waltz ◽  
Ramin M. Eskandari ◽  
Cynthia T. Welsh ◽  
Michael U. Antonucci
Keyword(s):  
Potential Role ◽  
Response To Treatment ◽  
Juvenile Xanthogranuloma ◽  
Imaging Features ◽  
Limited Information ◽  
Advanced Imaging ◽  
Systemic Involvement ◽  
The Central Nervous System ◽  
Infancy And Early Childhood

The authors report an unusual presentation of juvenile xanthogranuloma (JXG), a non–Langerhans cell histiocytosis of infancy and early childhood. This entity typically presents as a cutaneous head or neck nodule but can manifest with more systemic involvement including in the central nervous system. However, currently there is limited information regarding specific imaging features differentiating JXG from other neuropathological entities, with diagnosis typically made only after tissue sampling. The authors reviewed the initial images of a young patient with shunt-treated hydrocephalus and enlarging, chronic, extraaxial processes presumed to reflect subdural collections from overshunting, and they examine the operative discovery of a mass lesion that was pathologically proven to be JXG. Their results incorporate the important associated histological and advanced imaging features, including previously unreported metabolic activity on FDG PET. Ultimately, the case underscores the need to consider JXG in differential diagnoses of pediatric intracranial masses and highlights the potential role of PET in the initial diagnosis and response to treatment.

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