• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.220.3-220.3
• /
• 2003

Enantiomers of pindolol were prepared by chromatographic method. Racemic pindolol was derivatized with S-(-)-menthyl chloroformate((-)-MCF) forming its diastereomer, R-(+)-pindolol-(-)-MCF and S-(-)-pindolol-(-)-MCF. The diastereomer mixture was then chromatographically resolved to each diastereomer. Each diastereomer was further hydrolyzed with alkali to each enantiomer quantitatively. Racemization was not occurred in this process. Pindolol enantiomers were recovered producing good yield over 30% over all process.

• The Korean Journal of Pharmacology
• /
• v.28 no.1
• /
• pp.19-25
• /
• 1992

The effect of the nonbenzodiazepine anxiolytic, buspirone $(Buspar^R)$, a serotonin $(5-HT)_{1A}$ partial agonist, which also has dopamine $(DA)_2$ receptor antagonist properties, on prolactin and cortisol secretion was examined in eight normal male volunteers. The oral administration of buspirone (30 mg) significantly increased plasma prolactin concentrations but did not significantly increase plasma cortisol concentrations in this study. The oral administration of pindolol (30 mg), a beta adrenoceptor antagonist which is also a $5-HT_{1A}$ receptor antagonist, had no significant effect on basal prolactin or cortisol levels. Moreover, pretreatment with pindolol did not significantly inhibit the buspirone-induced increase in prolactin secretion. These preliminary data are suggestive that buspirone-induced prolactin secretion is not mediated via $5-HT_{1A}$ receptor activation.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.219.3-219.3
• /
• 2003

We describe here solid-extraction and derivatisation methods of ${\beta}$-adrenoceptor blocking drugs used for the treatment of various cardiovascular disorders such as hypertension, angina pectoris and cardiac arrhythmia: propranolol, metoprolol, sotalol, timolol, oxprenolol, alpranolol, atenolol, pindolol. Solid-extraction and derivatisation methods are described involving the use of Bond Elut Certify cartridges, MSTFA and MBTFA. Gas chromatographic-mass spectrometry analysis(GC/MS) was carried out select-ion monitroing mode. (omitted)

• Biomolecules & Therapeutics
• /
• v.12 no.3
• /
• pp.151-156
• /
• 2004

This study was carried out to evaluate the putative anxiolytic-1ike effects of the aqueous extracts of Sanjoin-tang (SJIT) and its ingredients using the elevated plus maze (EPM) test in mice. SJIT consists of five herbs, namely, Zizyphi Spinosi Semen (roasted), Glycyrrhizae Radix, Cnidii Rhizoma, Anemarrhenae Rhizoma, and Hoelen. The aqueous extracts of SJIT and each herbal drug were orally administered to ICR mice, 1 hr before evaluating behavioral activity in the EPM test, respectively. Repeated treatments (for 3 days) of the aqueous extract of SJIT (400 mg/kg) significantly increased time-spend in the open arms and arms entries into the open arms in the EPM test. Zizyphi Spinosi Semen (400 mg/kg), an ingredient of SJIT, significantly increased timespent in the open arms and arm entries into the open arms (P < 0.05). However, the other ingredient of SJIT did not show any anxiolytic-like behaviors. In addition, the anxiolytic-like effects of Zizyphi Spinosi Semen were blocked by pindolol (lO mg/kg), a $5-HT_{1A}$ receptor antagonist. These results suggest that Zizyphi Spinosi Semen (roasted) as an ingredient of SJIT plays a crucial anxiolytic role, and it acts via the serotonergic nervous system.

• Archives of Pharmacal Research
• /
• v.24 no.5
• /
• pp.402-406
• /
• 2001

Gas chromatographic method was investigated for the chiral separation of several $\beta$-blockeros(atenolol, betaxolol, bisoprolol, metoprolol and pindolol) using (-)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride as a chiral derivatizing agent for amino group. Prior to N-acylation, hydroxyl group was converted into O-silyl ethers by react with N-methyl-H-(taimethylsilyl)trifluoroacetamide. The reaction was selective and rapid and the diasteromeric derivatives were well separated by capillary gas chromatography. (R)-isomers were eluted faster than (S)-isomers when (-)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride was used as the chiral derivatizing agent. But in the opposite sequence when (+)-$\alpa$-methoxy-$\alpa$-(trifluoromethyl)phenylacetyl chloride was used. No racemization was found during the reaction.

• YAKHAK HOEJI
• /
• v.47 no.4
• /
• pp.200-205
• /
• 2003

The stability constants for the inclusion complexes between carboxymethyl-$\beta$-cyclodextrin (CM-$\beta$-CD) and five $\beta$-blockers, such as atenolol (ATE), bisoprolol (BIS), metoprolol (MET), pindolol (PIN) and propranolol (PRO) were determined by capillary electrophoresis. The magnitude of stability was decreased as following order; PRO＞MET＞BIS＞ATE＞PIN. Among them PRO showed the highest affinity towards CM-$\beta$-CD with stability constants of 383 and 371 $M^{-l}$ for (R)- and (S)-enantiomer, respectively. PIN enantiomers showed the lowest stability towards CM-$\beta$-CD, while the selectivity between (R)- and (S)-enantiomer was higher than any other tested $\beta$-blocker.r.

• Archives of Pharmacal Research
• /
• v.22 no.6
• /
• pp.608-613
• /
• 1999

Optimum conditions of chiral derivatization reaction of $\beta$-blockers (acebutolol, arotinolol, betaxolol, bisoprolol, celiprolol, metoprolol and pindolol) with (-)-menthyl chloroformate were investigated for the resolution by HPLC. With more than 30 times molar excess of (-)-methyl chloroformate chiral derivatization reactions were completed within one hour at room temperature except arotinolol and celiprolol. Diastereomeric derivatives of $\beta$-blockers were well resolved on the ODS column using acetonitrile-methanol-water as a mobile phase.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.6
• /
• pp.431-436
• /
• 2005

A high-performance liquid chromatographic method was validated for quantitation of nadolol in human plasma. Nadolol and internal standard, pindolol, were extracted with tert-butyl methyl ether after addition of 10 M sodium hydroxide solution. The analytes were separated on a reverse phased C18 column using a mobile phase consisting of 0.05 M ammonium phosphate monobasic buffer, acetonitrile and methanol (81: 17:2 v/v/v) and detected using a fluorescence detector (excitation wavelength 230 nm, emission wavelength 294 nm). The method was specific and sensitive enough to detect as low as 3 ng/mL of nadolol in human plasma. Linear calibration range was 3-150 ng/mL with correlation coefficient greater than 0.999. The overall accuracy was in the range of 96.8 to 103% and precision C.V.(%) 7.30 to 12.2%. The recovery was approximately 100% and stability was confirmed during storage and sample preparation. The present HPLC method was successfully applied to study bioavailability after oral administration of 80 mg of nadolol in healthy Korean subjects. The mean $AUC_{t}$ was $1968{\pm}397\;ng{\cdot}hr/mL$ and $C_{max}$ of $186{\pm}79.3\;ng/mL$ was reached at $3.5{\pm}0.76\;hr$. The mean $t_{1/2}$ of nadolol was $17.3{\pm}2.59\;hr$.

• Advances in Traditional Medicine
• /
• v.6 no.3
• /
• pp.186-195
• /
• 2006

The present study was carried out to determine the involvement of opioid and non-opioid receptor and the effect of pH and enzymes on the recently reported antinociceptive activity of aqueous extract of Corchorus olitorius (AECO) leaves using the abdominal constriction test. The extract was prepared by soaking the dried powdered leaves of Corchorus (C.) olitorius in distilled water overnight, and the supernatant obtained was considered as a stock solution with 100% concentration/ strength. The extract, administered subcutaneously in the concentrations/ strength of 10, 50 and 100%, was found to show a significant concentration-independent antinociception. The 50% concentration AECO were further used to study on the above mentioned parameters. The extract exhibited: significant (P < 0.05) decreased in activity when pre-treated (s.c.) against 10 mg/kg naloxonazine, bicuculine (10 mg/kg), phenoxybenzamine (10 mg/kg), 10 mg/kg pindolol, and 5 mg/kg mecamylamme, but not 10 mg/kg naltrindole, 10 mg/kg atropine, respectively; significant (P < 0.05) decreased in activity after pre-treatment against 10% a-amylase, but not 1 % protease or 10% lipase and; significant (P < 0.05) decreased in activity after exposure to alkaline condition (pH between 9 and 13) while maintaining the activity at acidic condition, respectively. The C. olitorius leaves antinociception, which involved, at least in part, activation of $\mu-opioid,\;\alpha-and\;\beta-adrenergic$, and nicotinic receptors, was found to decrease under alkaline condition and in the presence of $\alpha-amylase$.

• CELLMED
• /
• v.2 no.4
• /
• pp.38.1-38.6
• /
• 2012

The present study aimed to determine the possible mechanisms of the peripheral antinociception of the aqueous extracts of Dicranopteris linearis (AEDL), Melastoma malabathricum (AEMM) and Bauhinia purpurea (AEBP) leaves in mice. Briefly, the antinociceptive profile of each extract (300, 500, and 1000 mg/kg; subcutaneous (s.c.)), was established using the abdominal constriction test. A single dose (500 mg/kg) of each extract (s.c.) was pre-challenged for 10 min with various pain receptors' antagonists or pain mediators' blockers and 30 min later subjected to the antinociceptive assay to determine the possible mechanism(s) involved. Based on the results obtained, all extracts exerted significant (p < 0.05) antinociceptive activity with dose-dependent activity observed only with the AEMM. Furthermore, the antinociception of AEDL was attenuated by naloxone, atropine, yohimbine and theophylline; AEMM was reversed by yohimbine, theophylline, thioperamide, pindolol, reserpine, and 4-chloro-DL-phenylalanine methyl ester hydrochloride; and of AEBP was inhibited by naloxone, haloperidol, yohimbine and reserpine. In conclusion, the antinociceptive activity of those extracts possibly involved the activation of several pain receptors (i.e. opioids, muscarinic, ${\alpha}_2$-adrenergic and adenosine receptors, adenosine, H3-histaminergic and $5HT_{1A}$, dopaminergic receptors).