Pub Date : 2000-03-01DOI: 10.1211/146080800128735791
R. Archana, A. Namasivayam
The effect of an ethanolic extract of Ocimum sanctum on noise-stress-induced changes in immune parameters has been studied in albino rats. Acute noise stress caused leukopaenia, a significant increase in plasma corticosterone concentrations, and significant increases in thymus weight and cell count. It also caused a significant decrease in the antibody titre, and in spleen weight and cell count. There was no change in lymph node and adrenal gland weight, nor in inhibition of leukocyte migration. Pretreatment of the stressed group with the extract returned noise-stress-altered values to normal levels, indicating the stress-alleviating potential of Ocimum sanctum.
{"title":"Effect of Ocimum sanctum on Noise‐induced Changes in Immune Parameters","authors":"R. Archana, A. Namasivayam","doi":"10.1211/146080800128735791","DOIUrl":"https://doi.org/10.1211/146080800128735791","url":null,"abstract":"The effect of an ethanolic extract of Ocimum sanctum on noise-stress-induced changes in immune parameters has been studied in albino rats. Acute noise stress caused leukopaenia, a significant increase in plasma corticosterone concentrations, and significant increases in thymus weight and cell count. It also caused a significant decrease in the antibody titre, and in spleen weight and cell count. There was no change in lymph node and adrenal gland weight, nor in inhibition of leukocyte migration. Pretreatment of the stressed group with the extract returned noise-stress-altered values to normal levels, indicating the stress-alleviating potential of Ocimum sanctum.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"9 1","pages":"145-147"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82053305","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-03-01DOI: 10.1211/146080800128735782
S. Panda, A. Kar
The combined effects of three different plant extracts (Ashwagandha root, Guggulu gum and Bauhinia bark) on the regulation of thyroid function and on lipid peroxidation have been studied in laboratory mice. Daily administration of these extracts (1.4g kg−1 Ashwagandha, 0.2 g kg−1 Guggulu and 2.5g kg−1 Bauhinia) for 30 days enhanced serum concentrations of both thyroid hormones (thyroxine and triiodothyronine) without altering hepatic lipid peroxidation, indicating that these plant extracts, given in combination, stimulate thyroid function without hepatotoxic effects. The plant extracts also induced an increase in hepatic catalase activity, further suggesting the hepatoprotective nature of the extracts. These plant extracts might be used to formulate a drug for the treatment of hypothyroidism.
研究了三种不同植物提取物(Ashwagandha根、guguulu胶和紫荆皮)对小鼠甲状腺功能和脂质过氧化的联合调节作用。每天服用这些提取物(1.4g kg - 1 Ashwagandha, 0.2 g kg - 1 guguulu和2.5g kg - 1紫荆)30天，可以提高血清中甲状腺激素(甲状腺素和三碘甲状腺原氨酸)的浓度，而不会改变肝脏脂质过氧化，这表明这些植物提取物联合使用可以刺激甲状腺功能，而不会产生肝毒性作用。植物提取物还诱导肝脏过氧化氢酶活性的增加，进一步表明提取物的肝保护性质。这些植物提取物可用于配制治疗甲状腺功能减退症的药物。
{"title":"Combined Effects of Ashwagandha, Guggulu and Bauhinia Extracts in the Regulation of Thyroid Function and on Lipid Peroxidation in Mice","authors":"S. Panda, A. Kar","doi":"10.1211/146080800128735782","DOIUrl":"https://doi.org/10.1211/146080800128735782","url":null,"abstract":"The combined effects of three different plant extracts (Ashwagandha root, Guggulu gum and Bauhinia bark) on the regulation of thyroid function and on lipid peroxidation have been studied in laboratory mice. Daily administration of these extracts (1.4g kg−1 Ashwagandha, 0.2 g kg−1 Guggulu and 2.5g kg−1 Bauhinia) for 30 days enhanced serum concentrations of both thyroid hormones (thyroxine and triiodothyronine) without altering hepatic lipid peroxidation, indicating that these plant extracts, given in combination, stimulate thyroid function without hepatotoxic effects. The plant extracts also induced an increase in hepatic catalase activity, further suggesting the hepatoprotective nature of the extracts. \u0000 \u0000These plant extracts might be used to formulate a drug for the treatment of hypothyroidism.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"6 1","pages":"141-143"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81512924","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-03-01DOI: 10.1211/146080800128735746
M. Schlitzer, I. Sattler
We have recently described non-peptidic, non-prenylic bisubstrate analogues as novel farnesyltransferase inhibitors comprising three modules-a farnesylmimetic, a linker and an AAX-peptidomimetic substructure. In this study we replaced the originally used β-alanyl linker by several aliphatic and cyclic amino acids to investigate the effects on inhibitory potential of the stereochemistry of this central group. Whereas replacement of β-alanine by glycine did not affect inhibitory activity, all other modifications resulted in reduced activity. This result, which will be helpful for further development, shows that the bioactive conformation is none of those fixed by the rigid linkers.
{"title":"Non-peptidic, Non-prenylic Bisubstrate Farnesyltransferase Inhibitors, 4. Effect on Farnesyltransferase Inhibitory Activity of Conformational Restrictions in the Central Group","authors":"M. Schlitzer, I. Sattler","doi":"10.1211/146080800128735746","DOIUrl":"https://doi.org/10.1211/146080800128735746","url":null,"abstract":"We have recently described non-peptidic, non-prenylic bisubstrate analogues as novel farnesyltransferase inhibitors comprising three modules-a farnesylmimetic, a linker and an AAX-peptidomimetic substructure. In this study we replaced the originally used β-alanyl linker by several aliphatic and cyclic amino acids to investigate the effects on inhibitory potential of the stereochemistry of this central group. Whereas replacement of β-alanine by glycine did not affect inhibitory activity, all other modifications resulted in reduced activity. This result, which will be helpful for further development, shows that the bioactive conformation is none of those fixed by the rigid linkers.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"111 1","pages":"117-124"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79333633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-03-01DOI: 10.1211/146080800128735737
A. Kebriaeezadeh, A. Zarghi, R. Ahmadkhaniha, A. Khoddam, A. Ebrahimian
An HPLC method has been developed for simultaneous analysis of sulphamethoxazole (SMZ) and trimethoprim (TMP) in plasma from man. The detection limits for TMP and SMZ in plasma were 5 and 10ng mL−1, respectively. The average recovery for both compounds was 96% (approx.). The inter- and intra-day coefficients of variation of the assay were found to be less than 8%. The method is simple, sensitive and suitable for pharmacokinetic studies of sulphamethoxazole and trimethoprim.
{"title":"Simultaneous High‐Performance Liquid Chromatographic Determination of Sulphamethoxazole and Trimethoprim in the Plasma of Man","authors":"A. Kebriaeezadeh, A. Zarghi, R. Ahmadkhaniha, A. Khoddam, A. Ebrahimian","doi":"10.1211/146080800128735737","DOIUrl":"https://doi.org/10.1211/146080800128735737","url":null,"abstract":"An HPLC method has been developed for simultaneous analysis of sulphamethoxazole (SMZ) and trimethoprim (TMP) in plasma from man. The detection limits for TMP and SMZ in plasma were 5 and 10ng mL−1, respectively. The average recovery for both compounds was 96% (approx.). The inter- and intra-day coefficients of variation of the assay were found to be less than 8%. \u0000 \u0000 \u0000 \u0000The method is simple, sensitive and suitable for pharmacokinetic studies of sulphamethoxazole and trimethoprim.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"47 1","pages":"113-115"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78171656","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-03-01DOI: 10.1211/146080800128735728
K. Welham, M. Domin, K. Johnson, L. Jones, D. Ashton
Although much research has been completed on the application of matrix-assisted laser-desorption/ionization mass spectrometry (MALDI-MS) to the analysis of bacteria, no definitive studies have yet been performed on the analysis of fungi. Preliminary studies on the application of the MALDI-MS methodology, previously developed for the analysis of bacteria, to the analysis of intact fungal spores are described here. MALDI-MS and electrospray mass Spectrometry enable the analysis of high molecular-weight proteins, glycoproteins, oligosaccharides and oligonucleotides. Using MALDI-MS with bacteria has enabled the production of ‘fingerprints» of the intact cells; the ions observed are associated with the proteinaceous components of the cell wall. This study reports the adaptation of this technique to the direct analysis of fungal cells. Because of the large amount of carbohydrate in the fungal cell wall, the ions observed in the mass spectrometric experiments might be of carbohydrate origin. Penicillium spp., Scytalidium dimidiatum and Trichophyton rubrum have been studied in this preliminary investigation and all furnish individually distinctive spectra which seem to provide a profile of the cellular material with discrete peaks being observed over the mass range 2 to 13 kDa. The spectra obtained are reproducible within the method used but, as shown in our previous studies on bacteria, washing might selectively release components from the fungal cell wall.
{"title":"Matrix‐assisted Laser‐desorption/Ionization Time‐of‐flight Mass Spectrometry and its Application to the Analysis of Fungal Spores","authors":"K. Welham, M. Domin, K. Johnson, L. Jones, D. Ashton","doi":"10.1211/146080800128735728","DOIUrl":"https://doi.org/10.1211/146080800128735728","url":null,"abstract":"Although much research has been completed on the application of matrix-assisted laser-desorption/ionization mass spectrometry (MALDI-MS) to the analysis of bacteria, no definitive studies have yet been performed on the analysis of fungi. Preliminary studies on the application of the MALDI-MS methodology, previously developed for the analysis of bacteria, to the analysis of intact fungal spores are described here. \u0000 \u0000 \u0000 \u0000MALDI-MS and electrospray mass Spectrometry enable the analysis of high molecular-weight proteins, glycoproteins, oligosaccharides and oligonucleotides. Using MALDI-MS with bacteria has enabled the production of ‘fingerprints» of the intact cells; the ions observed are associated with the proteinaceous components of the cell wall. This study reports the adaptation of this technique to the direct analysis of fungal cells. Because of the large amount of carbohydrate in the fungal cell wall, the ions observed in the mass spectrometric experiments might be of carbohydrate origin. Penicillium spp., Scytalidium dimidiatum and Trichophyton rubrum have been studied in this preliminary investigation and all furnish individually distinctive spectra which seem to provide a profile of the cellular material with discrete peaks being observed over the mass range 2 to 13 kDa. The spectra obtained are reproducible within the method used but, as shown in our previous studies on bacteria, washing might selectively release components from the fungal cell wall.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"1 1","pages":"107-111"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77302515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-03-01DOI: 10.1211/146080800128735755
S. Anoopkumar‐Dukie, B. Glass, R. B. Walker, S. Daya
The effects of melatonin, a known free-radical scavenger, on paracetamol in the presence of UV irradiation was studied by use of HPLC. The experiments were performed in air and nitrogen. The results show that the rate of photodegradation of melatonin is faster in air than in nitrogen whereas that of paracetamol is similar in air and nitrogen. When the two drugs were combined, melatonin retarded the degradation of paracetamol for up to 6h in the presence of nitrogen. However, in the presence of air melatonin rapidly enhances the photodegradation of paracetamol. This study shows that a combination of melatonin and paracetamol in the presence of air and UV irradiation can lead to rapid inactivation of both agents, thus raising important concerns about the possible use of melatonin as sunscreen.
{"title":"Melatonin Alters the Photodegradation of Paracetamol","authors":"S. Anoopkumar‐Dukie, B. Glass, R. B. Walker, S. Daya","doi":"10.1211/146080800128735755","DOIUrl":"https://doi.org/10.1211/146080800128735755","url":null,"abstract":"The effects of melatonin, a known free-radical scavenger, on paracetamol in the presence of UV irradiation was studied by use of HPLC. The experiments were performed in air and nitrogen. \u0000 \u0000The results show that the rate of photodegradation of melatonin is faster in air than in nitrogen whereas that of paracetamol is similar in air and nitrogen. When the two drugs were combined, melatonin retarded the degradation of paracetamol for up to 6h in the presence of nitrogen. However, in the presence of air melatonin rapidly enhances the photodegradation of paracetamol. \u0000 \u0000This study shows that a combination of melatonin and paracetamol in the presence of air and UV irradiation can lead to rapid inactivation of both agents, thus raising important concerns about the possible use of melatonin as sunscreen.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"13 1","pages":"125-127"},"PeriodicalIF":0.0,"publicationDate":"2000-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73879807","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-02-01DOI: 10.1211/146080800128735683
X. Leval, Y. Henrotin, A. Labasse, J. Reginster, P. Neven, J. Delarge, F. Somers, B. Masereel, B. Pirotte, J. Dogné
Nimesulide, a non-steroidal anti-inflammatory drug and one of a promising class of selective COX-2 inhibitors, has a very interesting therapeutic profile. Unfortunately, it is poorly soluble in water, which leads to important difficulties in the formulation of injectable solutions. This problem can also affect the bioavailability of nimesulide. To increase the aqueous solubility of the drug a nimesulide-L-lysine salt was synthesized in our laboratory; its aqueous solubility was greater than that of nimesulide (solubility in purified water 7.5 mg mL−1, and 0.01 mg mL-1, respectively). The aim of this study was to compare the anti-inflammatory profiles of nimesulide and nimesulide-L-lysine salt in a two-step in-vitro investigation. First, we evaluated the COX-2 selectivity of the drugs by a method using purified COX-1 and COX-2 enzymes. In a second step we evaluated the effects of the drugs on the production of prostaglandin E2 (PGE2) and proteoglycan by chondrocytes from man. The results obtained confirmed the COX-2 selectivity of the two compounds. Nimesulide-L-lysine had the same anti-inflammatory profile as nimesulide on chondrocyte cultures and better water solubility. Nimesulide-L-lysine should, therefore, be used to prepare injectable preparations and should ameliorate bioavailability after oral treatments.
{"title":"Comparison of the effects of nimesulide and nimesulide-L-lysine on PGE2 production by COX-1 and COX-2 and on chondrocyte metabolism in-vitro","authors":"X. Leval, Y. Henrotin, A. Labasse, J. Reginster, P. Neven, J. Delarge, F. Somers, B. Masereel, B. Pirotte, J. Dogné","doi":"10.1211/146080800128735683","DOIUrl":"https://doi.org/10.1211/146080800128735683","url":null,"abstract":"Nimesulide, a non-steroidal anti-inflammatory drug and one of a promising class of selective COX-2 inhibitors, has a very interesting therapeutic profile. Unfortunately, it is poorly soluble in water, which leads to important difficulties in the formulation of injectable solutions. This problem can also affect the bioavailability of nimesulide. To increase the aqueous solubility of the drug a nimesulide-L-lysine salt was synthesized in our laboratory; its aqueous solubility was greater than that of nimesulide (solubility in purified water 7.5 mg mL−1, and 0.01 mg mL-1, respectively). \u0000 \u0000 \u0000 \u0000The aim of this study was to compare the anti-inflammatory profiles of nimesulide and nimesulide-L-lysine salt in a two-step in-vitro investigation. First, we evaluated the COX-2 selectivity of the drugs by a method using purified COX-1 and COX-2 enzymes. In a second step we evaluated the effects of the drugs on the production of prostaglandin E2 (PGE2) and proteoglycan by chondrocytes from man. The results obtained confirmed the COX-2 selectivity of the two compounds. Nimesulide-L-lysine had the same anti-inflammatory profile as nimesulide on chondrocyte cultures and better water solubility. \u0000 \u0000 \u0000 \u0000Nimesulide-L-lysine should, therefore, be used to prepare injectable preparations and should ameliorate bioavailability after oral treatments.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"22 1","pages":"83-87"},"PeriodicalIF":0.0,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74628633","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-02-01DOI: 10.1211/146080800128735719
C. Chaimbault, J. Bosc, C. Jarry, S. Daulouède, P. Vincendeau
One-step ring-annulation of 5-substituted 2-amino-2-oxazolines with diethyl ethoxymethy-lenemalonate yielded 2-substituted 6-carboethoxy-2,3-dihydro-5H-oxazolo[3,2-a]pyrimidin-5-ones. Under the same conditions 2-substituted 6-cyano-2,3-dihydro-5H-oxazolo[3,2-a]-pyrimidin-5-ones and the corresponding 2-ethyl(methylenecyanoacetate)-2-iminooxazo-lidines were obtained from ethyl ethoxymethylenecyanoacetate. Some of these compounds were evaluated in mice for antiparasitic activity.
{"title":"Synthesis and Preliminary Pharmacological Evaluation of New 6‐cyano‐2,3‐dihydro‐5H‐oxazolo[3,2‐a]pyrimidin‐5‐ones and 2‐ethyl(methylenecyanoacetate)‐2‐iminooxazolidines","authors":"C. Chaimbault, J. Bosc, C. Jarry, S. Daulouède, P. Vincendeau","doi":"10.1211/146080800128735719","DOIUrl":"https://doi.org/10.1211/146080800128735719","url":null,"abstract":"One-step ring-annulation of 5-substituted 2-amino-2-oxazolines with diethyl ethoxymethy-lenemalonate yielded 2-substituted 6-carboethoxy-2,3-dihydro-5H-oxazolo[3,2-a]pyrimidin-5-ones. Under the same conditions 2-substituted 6-cyano-2,3-dihydro-5H-oxazolo[3,2-a]-pyrimidin-5-ones and the corresponding 2-ethyl(methylenecyanoacetate)-2-iminooxazo-lidines were obtained from ethyl ethoxymethylenecyanoacetate. Some of these compounds were evaluated in mice for antiparasitic activity.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"168 1","pages":"101-105"},"PeriodicalIF":0.0,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80568770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-02-01DOI: 10.1211/146080800128735638
I. Charton, A. Mamai, C. Bennejean, P. Renard, P. Delagrange, P. Morgan, H. Howell, M. Gourdel-Martin, M. Viaud, G. Guillaumet
To discover analogues of melatonin with a longer half-life, novel non-indole analogues of the compound, in which the amide group of the side-chain has been reversed, have been prepared and evaluated in binding assays to determine their activity on melatonin receptors. The two most active compounds were those with the N-methylbutyramide side-chain. Butyramide and pentanoylamide side-chains resulted in similar affinities, irrespective of the skeleton tested whereas a propionamide side-chain led to loss of affinity. The biological actity of the molecules was more influenced by the length of the side-chain than by the nature of the skeleton, which had little effect. The results obtained show the relative importance of the length of the side-chain and of the nature of the skeleton in both the binding to and the activity on the melatonin receptor of the retroamide series.
{"title":"Synthesis and Biological Activity of New Melatonin Receptor Ligands","authors":"I. Charton, A. Mamai, C. Bennejean, P. Renard, P. Delagrange, P. Morgan, H. Howell, M. Gourdel-Martin, M. Viaud, G. Guillaumet","doi":"10.1211/146080800128735638","DOIUrl":"https://doi.org/10.1211/146080800128735638","url":null,"abstract":"To discover analogues of melatonin with a longer half-life, novel non-indole analogues of the compound, in which the amide group of the side-chain has been reversed, have been prepared and evaluated in binding assays to determine their activity on melatonin receptors. \u0000 \u0000 \u0000 \u0000The two most active compounds were those with the N-methylbutyramide side-chain. Butyramide and pentanoylamide side-chains resulted in similar affinities, irrespective of the skeleton tested whereas a propionamide side-chain led to loss of affinity. The biological actity of the molecules was more influenced by the length of the side-chain than by the nature of the skeleton, which had little effect. \u0000 \u0000 \u0000 \u0000The results obtained show the relative importance of the length of the side-chain and of the nature of the skeleton in both the binding to and the activity on the melatonin receptor of the retroamide series.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"15 1","pages":"49-60"},"PeriodicalIF":0.0,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79747063","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2000-02-01DOI: 10.1211/146080800128735647
V. Leclerc, N. Beaurain, P. Depreux, C. Bennejean, P. Delagrange, J. Boutin, D. Lesieur
A novel series of melatonin analogues based on the benzothiophene nucleus is described. In these compounds the methoxy group was replaced by electron-attracting groups such halogens (Br and Cl) with the aim of supplementing structure-affinity relationships on melatoninergic ligands. Target derivatives were prepared from the corresponding 4-halo-thiophenol. Some of these derivatives had high affinity for mt1 and MT2 receptors, almost as high as that of melatonin. These results prove that the methoxy group is not an essential requirement for binding to melatoninergic receptors.
{"title":"5-Halobenzothiophene Analogues of Melatonin: Synthesis and Affinity for mt1 and MT2 Receptors in Man","authors":"V. Leclerc, N. Beaurain, P. Depreux, C. Bennejean, P. Delagrange, J. Boutin, D. Lesieur","doi":"10.1211/146080800128735647","DOIUrl":"https://doi.org/10.1211/146080800128735647","url":null,"abstract":"A novel series of melatonin analogues based on the benzothiophene nucleus is described. In these compounds the methoxy group was replaced by electron-attracting groups such halogens (Br and Cl) with the aim of supplementing structure-affinity relationships on melatoninergic ligands. Target derivatives were prepared from the corresponding 4-halo-thiophenol. Some of these derivatives had high affinity for mt1 and MT2 receptors, almost as high as that of melatonin. \u0000 \u0000 \u0000 \u0000These results prove that the methoxy group is not an essential requirement for binding to melatoninergic receptors.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"24 1","pages":"61-65"},"PeriodicalIF":0.0,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87772958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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