A comparison of some pharmacological effects of naloxone and N-methylnaloxone in mice

1982 ◽  
Vol 60 (5) ◽  
pp. 715-719 ◽  
Author(s):  
K. Ramabadran ◽  
C. Suaudeau ◽  
J. J. C. Jacob
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Subcutaneous Administration ◽  
Intracerebroventricular Injection ◽  
Pharmacological Effects ◽  
Opioid Antagonists ◽  
Hot Plate ◽  
Two Factors ◽  
The Central Nervous System ◽  
Derivatives Of

The effects of N-methylnaloxone following subcutaneous and intracerebroventricular administrations on nociception were investigated using the hot plate technique. Unlike naloxone, subcutaneous administration of N-methylnaloxone did not enhance the nociceptive reactions. In contrast, intracerebroventricular injection of N-methylnaloxone produced antinociception and tremor. Compared with naloxone, N-methylnaloxone was very weak in precipitating the signs of abstinence in mice rendered acutely dependent on morphine. Two factors, poor penetration into the central nervous system and steric hindrance, might render N-methylnaloxone very weak and hence both these factors must be taken into consideration while analyzing the effects following quaternary derivatives of opioid antagonists.

SOME BASIC DERIVATIVES OF 6-CHLOROQUINAZOLINE AND PHTHALAZINE

1956 ◽  
Vol 34 (11) ◽  
pp. 1557-1561 ◽  
Author(s):  
Stanley O. Winthrop ◽  
Stella Sybulski ◽  
Roger Gaudry ◽  
Gordon A. Grant
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Physiological Action ◽  
The Central Nervous System ◽  
Derivatives Of ◽  
System Sodium

Basic derivatives of 6-chloroquinazoline and phthalazine have been synthesized and screened for their physiological action on the central nervous system. Sodium dialkylaminoalkoxides and the appropriate chlorobenzodiazine were brought together to yield basic ethers of 6-chloroquinazoline and phthalazine respectively. 1-(γ-Dimethylaminopropylamino)phthalazine was also prepared.

scholarly journals Isolation and partial characterization of methylated arginines from the encephalitogenic basic protein of myelin

1971 ◽  
Vol 123 (1) ◽  
pp. 69-74 ◽  
Author(s):  
G. S. Baldwin ◽  
P. R. Carnegie
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Ion Exchange ◽  
Human Brain ◽  
Conformational Changes ◽  
Basic Protein ◽  
The Central Nervous System ◽  
Derivatives Of ◽  
Exchange Behaviour

Two methylated derivatives of arginine were isolated from the encephalitogenic protein of myelin from the central nervous system. Evidence is presented for the proposed structures, ω-NN′-dimethylarginine and ω-N-monomethylarginine. In the encephalitogenic protein from human brain the proportion 1:6:10 for arginine:monomethylarginine:dimethylarginine residues was found to occur at position 107. Possible roles for the methylated arginine in conformational changes and altered ion-exchange behaviour are discussed.

scholarly journals Synthesis and pharmacological properties of 3-(2-methyl-furan-3-yl)-4-substituted-Δ2-1,2,4-triazoline-5-thiones

2008 ◽  
Vol 6 (1) ◽  
pp. 47-53 ◽  
Author(s):  
Agata Siwek ◽  
Monika Wujec ◽  
Maria Dobosz ◽  
Ewa Jagiełło-Wójtowicz ◽  
Anna Chodkowska ◽  
...  
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Carboxylic Acid ◽  
Acid Hydrazide ◽  
Pharmacological Properties ◽  
Pharmacological Effects ◽  
Carboxylic Acid Hydrazide ◽  
Wide Range ◽  
The Central Nervous System

AbstractBy the reaction of 2-methyl-furan-3-carboxylic acid hydrazide with isothiocyanates, 1-[(2-methyl-furan-3-yl)carbonyl]-4-substituted thiosemicarbazides 1 were obtained. Further cyclization with 2% NaOH led to the formation of 3-(2-methyl-furan-3-yl)-4-substituted-Δ2-1,2,4-triazoline-5-thiones 2. The pharmacological effects of 2 on the central nervous system in mice were investigated. Strong antinociceptive properties of the investigated derivatives were observed in a wide range of doses.

scholarly journals Research Progress on the Effect of Sphingosine Kinase 2 on Glioma

2021 ◽  
Vol 5 (6) ◽  
pp. 16-19
Author(s):  
Chunpeng Wang ◽  
Xiaohui Liu ◽  
Shiwen Guo
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Sphingosine Kinase ◽  
Immunohistochemical Method ◽  
Research Progress ◽  
Control Group ◽  
Sphingosine Kinase 2 ◽  
Two Factors ◽  
The Central Nervous System

Objective: The purpose of this study is to explore the role of sphingosine kinase 2 (SphK2) in the treatment of glioma, which is the most common primary tumor in the central nervous system. Methods: A total of 82 patients were included in this study, with 27 cases in the control group and 55 cases in the glioma group; the expressions of SphK2 and gp130 in the two groups were compared by immunohistochemical method, and the correlation between the two factors was analyzed. Results: Both SphK2 and gp130 were upregulated in the glioma group, and the two factors were significantly correlated. Conclusion: The high expression of SphK2 may play an important role in the occurrence, development, and diagnosis of glioma.

Stereoselective actions of S-nitrosocysteine in central nervous system of conscious rats

1997 ◽  
Vol 272 (5) ◽  
pp. H2361-H2368 ◽  
Author(s):  
R. L. Davisson ◽  
M. D. Travis ◽  
J. N. Bates ◽  
A. K. Johnson ◽  
S. J. Lewis
Keyword(s):  
Central Nervous System ◽  
Heart Rate ◽  
Nervous System ◽  
Intracerebroventricular Injection ◽  
Conscious Rats ◽  
Arterial Blood ◽  
Recognition Sites ◽  
Pressor Responses ◽  
The Central Nervous System ◽  
Intracerebroventricular Injections

This study examined whether the stereoselective actions of S-nitrosocysteine (SNC) in the central nervous system involves the activation of stereoselective SNC recognition sites. We examined the effects produced by intracerebroventricular injection of the L- and D-isomers of SNC (L- and D-SNC) on mean arterial blood pressure, heart rate, and vascular resistances in conscious rats. We also examined the hemodynamic effects produced by intracerebroventricular injections of 1) L-cystine, the major non-nitric oxide (NO) decomposition product of L-SNC, 2) the parent thiols L- and D-cysteine, and 3) the bulky S-nitrosothiol L-S-nitroso-gamma-glutamylcysteinylglycine [L-S-nitrosoglutathione, (L-SNOG)]. Finally, we examined the decomposition of L- and D-SNC and L-SNOG to NO on their addition to brain homogenates. The intracerebroventricular injection of L-SNC (250-1,000 nmol) produced falls in mean arterial pressure, increases in heart rate, and a dose-dependent pattern of changes in hindquarter, renal, and mesenteric vascular resistances. The intracerebroventricular injections of D-SNC, L-cystine, and L-SNOG produced only minor effects. The intracerebroventricular injection of L-cysteine produced pressor responses and tachycardia, whereas D-cysteine was inactive. L- and D-SNC decomposed equally to NO on addition to brain homogenates. L-SNOG decomposed to similar amounts of NO as L- and D-SNC. These results suggest that SNC may activate stereoselective SNC recognition sites on brain neurons and that S-nitrosothiols of substantially different structure do not stimulate these sites. These recognition sites may be stereoselective membrane-bound receptors for which L-SNC is the unique ligand.

The Functions of the Corpus Allatum in Rhodnius Prolixus (Hemiptera)

1948 ◽  
Vol 25 (1) ◽  
pp. 1-15
Author(s):  
V. B. WIGGLESWORTH
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Juvenile Hormone ◽  
Adult Female ◽  
Corpus Allatum ◽  
Relative Importance ◽  
Egg Development ◽  
Mature Adult ◽  
Two Factors ◽  
The Central Nervous System

Two factors are involved in the control of metamorphosis in Rhodnius: (a) The corpus allatum of the 5th-stage nymph no longer secretes the juvenile hormone (inhibitory hormone). The latent imaginal characters can thus be realized. (b) The corpus allatum in the 5th-stage nymph, particularly in the later stages of moulting, actively favours the production of imaginal characters. The evidence suggests that this activity (b) consists, not in the secretion of a metamorphosis promoting hormone favouring adult differentiation in the tissues directly, but in the elimination of the small quantities of juvenile hormone persisting in the blood and tissues. If we suppose that these two factors differ in relative importance in different insects we may perhaps have the basis for a theory of metamorphosis applicable to all groups of insects. The corpus allatum of the mature adult Rhodnius again begins to secrete the juvenile hormone; and the juvenile hormone of the 4th-stage nymph will induce egg development in the adult female. It is probable that the yolk-forming hormone and the juvenile hormone are identical. The sequence in the secretory activities of the corpus allatum, and so the number of instars, is controlled by some other centre, perhaps in the central nervous system.

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