Structure-function relations and site of action of apamin, a neurotoxic polypeptide of bee venom with an action on the central nervous system

Biochemistry ◽  
1975 ◽  
Vol 14 (11) ◽  
pp. 2521-2525 ◽  
Author(s):  
Jean P. Vincent ◽  
Hugues Schweitz ◽  
Michel Lazdunski
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Structure Function ◽  
Bee Venom ◽  
Site Of Action ◽  
The Central Nervous System

Effects of Certain Indole Amines on Electrical Activity of the Nervous System

1956 ◽  
Vol 185 (3) ◽  
pp. 601-606 ◽  
Author(s):  
Alan G. Slocombe ◽  
Hudson Hoagland ◽  
Lillian S. Tozian
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Electrical Activity ◽  
Lysergic Acid ◽  
Subcortical Structures ◽  
Albino Rat ◽  
Site Of Action ◽  
The Central Nervous System ◽  
Recovery From Anesthesia ◽  
The Brain

Lysergic acid diethylamide (LSD), 5-hydroxytryptamine, and adrenochrome were shown to have properties similar to epinephrine in their effects on the spontaneous electrical activity in the brain of the albino rat. The effects of these drugs were shown to be determined by the type of anesthetic used. In Pentothal-anesthetized animals, profound reduction of the electrical activity in both frequency and amplitude was found in response to these drugs, while in ether-anesthetized animals there was no significant effect. There was a tendency for LSD to increase electrical activity when injected following recovery from anesthesia. The significance of this differential response is discussed with respect to structures in the central nervous system primarily affected by ether and Pentothal, and it is suggested that the site of action of these compounds is in Pentothal-sensitive nonspecific pathways. The site of the depressive action of these drugs with Pentothal is further defined by the fact that both cortical and subcortical structures were equally affected, while respiratory and cardio-regulatory centers were not significantly depressed. This implicates one of the lower nonspecific centers with widespread cortical and subcortical projections.

scholarly journals SITE OF ACTION OF TRANS-π-OXOCAMPHOR IN THE CENTRAL NERVOUS SYSTEM OF THE CAT

1964 ◽  
Vol 14 (2) ◽  
pp. 229-230 ◽  
Author(s):  
HIROSHI KUMAGAI ◽  
FUMINORI SARAI ◽  
TAKEHIKO HUKUHARA ◽  
YOSHIAKI SAJI ◽  
SUEHIRO NAKANISHP ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Site Of Action ◽  
The Central Nervous System

scholarly journals A Novel Prodrug Approach for Central Nervous System-Selective Estrogen Therapy

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4197 ◽  
Author(s):  
Katalin Prokai-Tatrai ◽  
Laszlo Prokai
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Estrogen Therapy ◽  
High Concentration ◽  
Beneficial Effects ◽  
Non Invasive ◽  
Site Of Action ◽  
The Central Nervous System ◽  
And Gender ◽  
Preclinical Animal Models

Beneficial effects of estrogens in the central nervous system (CNS) results from the synergistic combination of their well-orchestrated genomic and non-genomic actions, making them potential broad-spectrum neurotherapeutic agents. However, owing to unwanted peripheral hormonal burdens by any currently known non-invasive drug administrations, the development of estrogens as safe pharmacotherapeutic modalities cannot be realized until they are confined specifically and selectively to the site of action. We have developed small-molecule bioprecursor prodrugs carrying the para-quinol scaffold on the steroidal A-ring that are preferentially metabolized in the CNS to the corresponding estrogens. Here, we give an overview of our discovery of these prodrugs. Selected examples are shown to illustrate that, independently of the route of administrations and duration of treatments, these agents produce high concentration of estrogens only in the CNS without peripheral hormonal liability. 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED) has been the best-studied representative of this novel type of prodrugs for brain and retina health. Specific applications in preclinical animal models of centrally-regulated and estrogen-responsive human diseases, including neurodegeneration, menopausal symptoms, cognitive decline and depression, are discussed to demonstrate the translational potential of our prodrug approach for CNS-selective and gender-independent estrogen therapy with inherent therapeutic safety.

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