Spasmolytics,

Dimethylaminoethyl-2,4,6-trimethoxybenzoates and similar esters are useful as spasmolytics and in relieving indigestion (180). Bis-chromonyl compounds derived from phloroglucinol are valuable in the treatment of asthma (see Antiasthmatic agents) (181). 

OC-Bisabolol. a-Bisabolol (99) occurs in camomile flowers and has been shown to be the main antiphlogistic and spasmolytic component of the European medicinal plant. The use of bisabolol is recommended mainly for its pharmacodynamic properties in cosmetic preparations for skin protection. 

Salvia is one of the most important genera of the Family Lamiaceae. Several species of salvia ai e used in folk medicine as antiseptics, astringents and spasmolytics [3]. 

According to Nyman the pharmacological action of hyoscine is considerably modified in the quaternary compounds of the alkaloid, e.g., the inhibiting action on salivary secretion is greatly increased in the methonitrate, as is also the spasmolytic activity, but the mydriatic action is unchanged and the central sedative activity disappears. 

Comparable figures for a satisfactory range of substances tested as spasmolytics cannot be provided as authors state their results in different ways. The following short series is taken from Burtner and Cusic s... 

The activities are expressed as reciprocal functions and are referred to No. 7 as unity, so that the smaller the number the greater the activity. The results with Nos. 3 to 7 indicate that the esterifying acid has considerable influence both on the nature of the action and its intensity. None of the amino-alcohols used matches tropine as a source of spasmolytic action of the neurotropic type. 

It has been stated already (atropine, p. 112) that there are two types of spasmolytic drug, the neurotropic, typified by atropine, and the musculo-tropic or myotropic to which papaverine belongs. In laboratory work the two types are usually tested against spasm induced by acetylcholine and... 

Reviews of recent work on spasmolytic drugs have been published by Raymond and by Blicke, and a detailed account of the action of papaverine and its derivatives, including laudanosine and laudanine with numerous references to literature is given by Krueger, Eddy and bumwalt. ... 

In a search for new spasmolytics, Heilbron and Hey and their co-workers synthesized a number of pyridylquinolines by coupling diazotized arainoquinolines with pyridine. Pyridine has also been substituted by the 3-pyridyl radical in the Gomberg reaction, the 2-and 3-substituted products being obtained in 55 and 5% yield, respectively, together with a third product obtained in 20% yield w hich w as tentatively formulated as the 4-isomer. The same radical w as coupled with 4-methyl- and 4-ethyl-pyridine and gave in each case mixtures of the twm possible substitution products in which the radical had coupled predominantly with the carbon atom of pyridine adjacent to the alkyl substituent, as showm in Eq. (19). ... 

Dihydro-1,3-oxazines have been suggested as analgesics,sedatives and spasmolytics/ and fungicides. ... 

The simplification of the local anesthetic phaimacophore of cocaine to an aryl substituted ester of ethanolamine has been described previously. Atropine (S2) is a structurally closely related natural product whose main biologic action depends on inhibition of the parasympathetic nervous system. Among its many other actions, the compound exerts useful spasmolytic effects. 

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). ... 

Inclusion of a second nitrogen atom in the side chain seemingly increases the spasmolytic effect of the benzhydrol derivatives. Alkylation of the benzdryl chloride (9) with the sodium... 

Acylation of benzamidoxlme (144) with chloropropionyl chloride gives the 0-acylated derivative (145). Reaction of that intermediate with diethylamine serves first to cyclize the molecule to the 1,2,4-oxadiazole heterocycle subsequent displacement of the halogen on the side chain gives oxolamine (146),a drug with antltussive and spasmolytic activity. 

One of the few nonnitrogenous compounds to show spasmolytic activity is a rather simple chromone. Acylation of the phenolic ketone, 31, with the half ester-half acid chloride from oxalic... 

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... 

Spasmolytic. A drug that inhibits the contraction of intestinal smooth muscle. 

DHPs are potent arterial vasodilators. They act on resistance vessels and therefore reduce peripheral vascular resistance, lower arterial blood pressure, and antagonize vasospasms in coronary or peripheral arteries. By reducing afterload, DHPs also reduce cardiac oxygen demand. Together with their vascular spasmolytic effect, this explains most of the beneficial actions of DHPs in angina pectoris. Most DHPs are only licensed for the therapy of hypertension, some of them also for the treatment of angina pectoris and vasospastic (Prinzmetal) angina. 

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