Anxiolytic agents

In 2000, Simig et al. began to conduct structure activity relationships on 25 by employing the Pictet-Gams reaction. Compound 25 had been identified as an anxiolytic agent that does not show sedative side-effects. ... 

The anxiolytic agent buspirone (131) is notable for the fact that it does not interact with the receptor for the benzodiazepines. This difference in biochemical pharmacology is reflected in the fact that buspirone (131) seems to be devoid of some of the characteristic benzodiazepine side effects. The spiran function is apparently not required for anxiolytic activity. Alkylation of 3,3-dimethylglutarimide with dichlorobutane in the presence of strong base yields the intermedi-... 

Anxiolytic agents, pyrido[l,2-a]benzimida-zoles as, 36 (1999) 169 Aromatase inhibition and breast cancer, 26 (1989) 253 33 (1996) 147 Arthritis neurokinin receptors in, 43 (2005) 53... 

Replacement of the methylene group in 95 by oxygen results in yet another subtle qualitative change in CNS activity. The products of this replacement, such as 104 and 111, are characterized as anxiolytic agents. In the synthesis of 104 we find yet a different approach to the amidine function, beginning with reaction of 2-chloronitrobenzene with... 

The medicinal Lamiaceae, with about 250 species, represents a vast source of material to explore when looking for anxiolytic agents of clinical value. Among these medicinal species are Scutellaria baicalensis Georgi and Leonotis nepetifolia, the properties of which are described here. 

Thus, the evidence that stress, and the stress hormone corticosterone, may cause changes in hippocampal structure, hippocampal connections, and changes in gene and protein expression, suggest that viable targets of anxiolytic agents are cellular signaling pathways involved in neuroplasticity and the maintenance of cellular resilience. 

Quaglia, M. G., Farina, A., Bossu, E., and Dell aquila, C. (1995). Analysis of non-benzodiazepinic anxiolytic agents by capillary zone electrophoresis. /. Pharm. Biomed. Anal. 13, 505 — 509. 

The development of the benzodiazepine class of drugs for the treatment of a variety of neurological indications has proven to be an outstanting success story in the field of chemotherapy. However, these compounds often produce undesirable side effects when used as anti-anxiety or hypnotic agents. These side effects include sedation, physical dependence, amnesia, muscle relaxation, and ethanol potentiation. The development of a benzodiazepine receptor-based anxiolytic agent devoid of these side effects would constitute a major advance in the field and has been the focus of significant research efforts [284]. 

Fusion of an additional heterocyclic ring onto a benzodiazepine is well known to considerably increase potency. This increase in potency is apparently maintained when the benzene ring is replaced by thiophene. Thiophene aminoketone 161 is converted to the benzodiazepine analogue 164 via chloroacetamide 162 and then glycine derivative 163 by the same sequence as that used in the benzene series. Treatment of the product 164 with phosphorus pentasulfide gives the thio-amide 165 reaction of that intermediate with hydrazine leads to the amino amidine 166. Condensation of this with ethyl orthoacetate gives the anxiolytic agent brotizolam (167) [31]. 

Abstract Pharmacogenetics as a field of research is increasing the basis of knowledge on the use of psychotropics in different ethnic patient populations. This chapter summarizes cur-rentknowledge on the metabolism of anxiolytic agents with emphasis on pharmacogenetics and ethnic variations in drug responses. 

Buspirone (BuSpar) is the first example of a class of anxiolytic agents that can relieve some symptoms of anxiety in doses that do not cause sedation. Buspirone is structurally unrelated to existing psychotropic drugs. 

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