A new ion-exchanger type chiral stationary phase for high-performance liquid chromatography was prepared. The synthetic protocol is based on derivatization of silica with (3-iodopropyl)trimethoxysilane in the first step followed by immobilization of strychnine via quaternization of nitrogen atom of the alkaloid strychnine. The synthesized chiral stationary phase was chromatographically characterized. The main effort was headed towards the evaluation of the enantioselectivity of the novel sorbent. For that purpose a set of suitable chiral probes, specifically, binaphthyl derivatives, was employed. The influence of methanol content, concentration of aqueous ammonium acetate buffer, and its pH on retention factors, separation selectivity, and resolution of the atropoisomers of the mentioned chiral solutes was studied in detail. It was demonstrated that the new chiral stationary phase was capable to separate atropoisomers of four out of seven testing compounds. Despite the strong influence of the above mentioned variables on retention, their impact on selectivity and resolution was rather moderate. Concerning retention mechanism, it seems that electrostatic interaction between the positively charged quaternary nitrogen of the chiral stationary phase and anionic solute participates significantly in the retention process.

• Klíčová slova
• Alkaloid, Binaphthyl derivatives, Chiral separation, Chiral stationary phase, Strychnine,
• MeSH
• acetáty chemie   MeSH
• methanol chemie   MeSH
• stereoizomerie MeSH
• strychnin chemie   MeSH
• vysokoúčinná kapalinová chromatografie přístrojové vybavení   metody   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• acetáty MeSH
• ammonium acetate MeSH Prohlížeč
• methanol MeSH
• strychnin MeSH

• Klíčová slova
• RESPIRATION/pharmacology *, STRYCHNINE/pharmacology *,
• MeSH
• dýchání farmakologie   MeSH
• plicní ventilace * MeSH
• strychnin farmakologie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• strychnin MeSH

The interaction of strychnine (1 mg/kg egg weight), glycine (100 mg/kg egg weight) and GABA (103 mg/kg egg weight) on spontaneous motor activity recorded by the method of Kovach (1970) in intact eggs was studied in chick embryos from the 11th to 21st day of incubation. In 11- and 13-day embryos, neither of the amino acids influenced strychnine activation of spontaneous motility. From the 15th incubation day, strychnine activation was distinctly affected by both amino acids, but the maximum effect was observed on the 19th day. Glycine had a stronger inhibitory effect, since it prevented strychnine convulsions from developing, whereas GABA only modified them. It can be concluded from the results that glycine-sensitive and GABA-sensitive mechanisms of embryonal spontaneous motility do not begin to take effect in chick embryos until the 15th day of incubation.

• MeSH
• aminobutyráty farmakologie   MeSH
• GABA farmakologie   MeSH
• glycin farmakologie   MeSH
• kuřecí embryo účinky léků   MeSH
• lékové interakce MeSH
• pohybová aktivita účinky léků   MeSH
• strychnin farmakologie   MeSH
• zvířata MeSH
• Check Tag
• kuřecí embryo účinky léků   MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• aminobutyráty MeSH
• GABA MeSH
• glycin MeSH
• strychnin MeSH

Activation of spontaneous motility produced by the systemic administration of strychnine (1 mg/kg egg weight) and picrotoxin (1 mg/kg egg weight) was studied in 13- and 17-day-old chick embryos. In both cases the effect was studied in normal embryos, in embryos decapitated 1, 24 and 48 hours previously and in embryos decapitated on the 2nd day of incubation at stage 11-13 according to Hamburger and Hamilton (1951). At 13 days, both substances had the same short-term activating effect on the controls and all the decapitated embryos. This result is evaluated as further evidence of non-participation of the supraspinal component in the spontaneous motility of chick embryos before the 15th day of incubation. In 17-day-old decapitated embryos, strychnine and picrotoxin activation of spontaneous motility was significantly smaller than in the controls. From a comparison of activation by strychnine and picrotoxin in normal and chronically decapitated embryos it was deduced that a spinal and a supraspinal component participated in their effect. The activating effect of strychnine and picrotoxin in 17-day-old embryos was found to be mediated largely by supraspinal factors.

• MeSH
• chemická stimulace MeSH
• hlava chirurgie   MeSH
• kuřecí embryo fyziologie   MeSH
• mícha embryologie   MeSH
• mozek embryologie   MeSH
• pikrotoxin farmakologie   MeSH
• pohyb účinky léků   MeSH
• strychnin farmakologie   MeSH
• zvířata MeSH
• Check Tag
• kuřecí embryo fyziologie   MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• pikrotoxin MeSH
• strychnin MeSH

The longitudinal development of spontaneous motility in chick embryos was studied by Kovach's method (Kovach 1970) from the 10th day of incubation up to hatching, in completely intact eggs. From the 10th to 12th day of incubation, very low amplitude movements of a burst character predominated in spontaneous motility. From the 13th day, both low and high amplitude movements could be distinguished. From the 18th day, high amplitude movements alternating with intervals of motor inactivity preponderated. This discontinuous motility, which was most pronounced on the 20th day of incubation, changed to periodic strong hatching movements. Reduction of spontaneous motility after the 17th day of incubation was not confirmed. Strychnine already activated spontaneous motility in 11-day embryos, but typical convulsions did not appear until the 15th incubation day. With picrotoxin, motility was likewise stimulated in 11-day embryos and paroxysmal activation did not occur until the 15th incubation day. In older embryos, convulsions were gradually succeeded by a continuous increase in spontaneous motility. The effect of picrotoxin had a much longer latent period than the effect of strychnine.

• MeSH
• časové faktory MeSH
• chemická stimulace MeSH
• kuřecí embryo fyziologie   MeSH
• pikrotoxin farmakologie   MeSH
• pohyb účinky léků   MeSH
• strychnin farmakologie   MeSH
• zvířata MeSH
• Check Tag
• kuřecí embryo fyziologie   MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• pikrotoxin MeSH
• strychnin MeSH

• MeSH
• benzen farmakologie   MeSH
• elektroencefalografie MeSH
• kočky MeSH
• mozková kůra účinky léků   MeSH
• periodicita MeSH
• retikulární formace účinky léků   MeSH
• strychnin farmakologie   MeSH
• xyleny farmakologie   MeSH
• zvířata MeSH
• Check Tag
• kočky MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• benzen MeSH
• strychnin MeSH
• xyleny MeSH

The convulsant action of strychnine was studied in 310 male albino rats, aged 3 to 25 days. Doses of 0.25-4 mg/kg were administered intraperitoneally and the animals were observed for 30 min. Generalized tonic-clonic seizures involving also tonic hindlimb extension occurred in all age groups. The convulsant effects of strychnine increased from day 3 to day 18, and decreased again from day 25, as indicated by the incidence and latencies of seizures. Lethal effects did not occur before day 12. Hyperactivity was seen as the first sign of strychnine action in rats during the first week of life, automatisms predominating in 18-day-old animals. Electroencephalographic study in 30 rat pups with implanted electrodes demonstrated an extremely poor electro-clinical correlation.

• MeSH
• elektroencefalografie MeSH
• implantované elektrody MeSH
• injekce intraperitoneální MeSH
• konvulziva aplikace a dávkování   toxicita   MeSH
• krysa rodu Rattus MeSH
• potkani Wistar MeSH
• stárnutí MeSH
• strychnin aplikace a dávkování   toxicita   MeSH
• vztah mezi dávkou a účinkem léčiva MeSH
• záchvaty chemicky indukované   mortalita   MeSH
• zadní končetina MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• konvulziva MeSH
• strychnin MeSH

It has been shown previously that the third extracellular loop (o3) and its vicinity play a critical role in allosteric modulation at muscarinic acetylcholine receptors (mAChRs) (Ellis et al., 1993; Krejçí and Tuçek, 2001; Buller et al., 2002). In this study interaction of four chemically related substances (strychnine, its dimethoxy derivate brucine, precursor for synthesis of strychnine Wieland-Gumlich aldehyde (WGA), and precursor for synthesis of alcuronium propargyl-WGA) with orthosteric antagonist N-methylscopolamine (NMS) was investigated on the M3 subtype of mAChRs mutated at the o3 loop.

• MeSH
• alosterická regulace MeSH
• asparagin MeSH
• konformace proteinů MeSH
• mutageneze cílená MeSH
• N-methylskopolamin farmakologie   MeSH
• prolin MeSH
• receptory muskarinové chemie   účinky léků   fyziologie   MeSH
• serin MeSH
• strychnin farmakologie   MeSH
• substituce aminokyselin MeSH
• threonin MeSH
• valin MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• asparagin MeSH
• N-methylskopolamin MeSH
• prolin MeSH
• receptory muskarinové MeSH
• serin MeSH
• strychnin MeSH
• threonin MeSH
• valin MeSH

• MeSH
• diazepam terapeutické užití   MeSH
• epilepsie chemicky indukované   farmakoterapie   MeSH
• krysa rodu Rattus MeSH
• strychnin antagonisté a inhibitory   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• diazepam MeSH
• strychnin MeSH

• MeSH
• akustická stimulace MeSH
• evokované potenciály účinky léků   MeSH
• krysa rodu Rattus MeSH
• počítače MeSH
• psi MeSH
• sluchové korové centrum fyziologie   MeSH
• strychnin farmakologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• psi MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• strychnin MeSH