Spasmolytic agent

A further simplification of the requirements for activity came from the preparation of two spasmolytic agents that completely lack the aromatic ring. Thus, double alkylation of phenylace-tonitrile (54) with 1,5-dibromopentane leads to the corresponding cyclohexane (55). This intermediate is then saponified and the resulting acid (56) esterified with w,w-diethylethanolamine. Catalytic reduction of the aromatic ring affords dicyclonine (51). ... 

Papaverine (107) is among the host of minor alkaloids that have been isolated from opium. The compound is distinct in its biologic activity from many of the other opium constituents in that it does not exhibit any analgesic activity. Instead, papaverine acts as a nonspecific spasmolytic agent. As such, it has found... 

Treatment of symptomatic diverticular disease of the colon is aimed at the relief of symptoms and the prevention of major complications. The efficacy of fiber supplementation and of anticholinergic and spasmolytic agents remains controversial. Antibiotics are commonly used in the treatment of inflammatory complications of diverticular disease. Data from open labelled and randomized controlled trials do suggest the efficacy of rifaximin in obtaining symptomatic relief in patients with diverticular disease. Approximately 30% therapeutic gain compared to fiber supplementation only can be expected after one year of intermittent treatment with rifaximin. Considering the safety and tolerability of rifaximin, this drug can be recommended for patients with symptomatic uncomplicated diverticular disease. 

The observed hypermotility of the sigmoid colon in many symptomatic patients provides the rationale for using anticholinergic drugs and spasmolytic agents [25]. However, the efficacy of these agents has never been clearly documented in randomized controlled trials [3,24],... 

Tribulus terrestsis L. Ci Hi Li (Calthrop) (fruit) Glycosides tribuloside, astragalin, harmane, harmine.33 Anticonvulsive, a spasmolytic agent. 

After deglucosylation, the pathway proceeds through a 4,21-Dehydrogeissoschizine derivative to ajmalicine (an a-Blocking spasmolytic agent, used for tinnitus and cranial trauma with an ergot derivative). If cyclization occurs between C-17 and C-18, the yohimbine nucleus is produced, whose derivatives include the Rauvolfia alkaloids reserpine and resdnnamine (antihypertensive activity). Ajmaline, formerly used as an antiarrythmic, also occurs in Rauvolfia species, and several of the enzymes in the pathway have been isolated. Recent considerations suggest that the C-16-C-5 bond may be formed before the N-4-C-21 bond (Fig. 38). 

Skeletal muscle relaxants fall into three major categories those that reduce spasticity, those that cause neuromuscular blockade and those that work at the cellular level. Spasmolytic agents (e.g. metho-carbamol, guaifenesin) act centrally whereas neuromuscular blockers (e.g. succinylcholine (suxamethonium), pancuronium, atracurium) act at the neuromuscular end plate to produce muscular relaxation. Dantrolene falls into the third category and acts within the muscle cell itself to produce relaxation. 

In vitro studies with the spasmolytic agent chlorphencyclan (117a) and its silicon analogue silachlorphencyclan (117b) on the isolated guinea-pig ileum also revealed a... 

Other compounds in this group, viz. 3-alkyl-2,3-dihydro-6//-l, 3,4-selenadiazines (215), are useful as spasmolytic agents. They can be synthesized by the cyclocondensation of 2-halogenoalkanones with selenosemicarbazides (214) (Equation (50)) <90EGP281582,9lCZ36i>. 

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