Tag: 323.8591

Pre-treatment of BALB/c mice with a centrally acting serotonin antagonist (Cyproheptadine) reduces mortality from Boophone Disticha poisoning was written by Mutseura, M.;Tagwireyi, D.;Gadaga, L. L.. And the article was included in Clinical Toxicology in 2013.Related Products of 969-33-5 This article mentions the following:

Crude extracts of Boophone disticha are used in Southern African traditional medical practice for the management of various illnesses and conditions and have also been abused for their claimed euphoric and hallucinogenic effects. Unfortunately, ingestion of Boophone disticha has resulted in toxicity and death. The results of a recent acute toxicity study in a rat model insinuated that central nervous system (CNS) serotonin overdrive could be the cause of toxicity in B. disticha poisoning. The present work sought to test that hypothesis by investigating whether pre-treatment of B. disticha poisoned BALB/c mice with the CNS acting serotonin antagonist, cyproheptadine, has a dose-dependent protective effect on toxicity and mortality. A hydroethanolic extract of B. disticha was used in all the experiments Five groups each with 10 animals were constituted as follows; a neg. control group (received 10 mL/kg Normal Saline), a pos. control group (received 375 mg/kg of the B. disticha extract), and three test groups each receiving 10 mg/kg, 15 mg/kg and 20 mg/kg cyproheptadine i.p. 15 min before oral gavage administration of 375 mg/kg B. disticha extract resp. The Functional Observational Battery was used to evaluate neurobehavioral and physiol. changes resulting from toxicity of the plant extract The mice were then placed in an open field for another five minutes and the number of rearings and border crossings were counted and recorded. Gait abnormalities, involuntary motor movements, mobility, arousal and stereotypical behavior were also scored according to predefined criteria. All open field investigations were recorded electronically using a LABTEC Webcam and results were later analyzed and recorded by one of the group members. All results were entered on data collection forms. Time to death (survival time) was considered as the time period from dosage with Boophone disticha to time of death. The study follow up period was 7 days and those mice that were alive at the end of the 7 day follow-up period were considered as having survived the poisoning episode. The Kaplan Meier plot and Log-rank test were used to compare differences in mortality and median time to death for mice in the 5 treatment groups. We found that cyproheptadine pre-treatment led to a dose-dependent decrease in mortality from 80% in the group not pre-treated with cyproheptadine, to 30% in the 15 and 20 mg/kg cyproheptadine pre-treated groups (n = 10 per group, p < 0.05). There was also a dose-dependent increase in median survival times amongst the groups (p < 0.0001). Pre-treatment with cyproheptadine also resulted in a decrease of other toxic symptoms associated with Boophone disticha. We conclude that cyproheptadine has a dose-dependent protective effect on mortality and toxicity produced by exposure to Boophone disticha in our mouse model of toxicity. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Related Products of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Related Products of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cyproheptadine displays preclinical activity in myeloma and leukemia was written by Mao, Xinliang;Liang, Sheng-ben;Hurren, Rose;Gronda, Marcela;Chow, Sue;Xu, G. Wei;Wang, Xiaoming;Zavareh, Reza Beheshti;Jamal, Nazir;Messner, Hans;Hedley, David W.;Datti, Alessandro;Wrana, Jeff L.;Zhu, Yuanxiao;Shi, Chang-xin;Lee, Kyle;Tiedemann, Rodger;Trudel, Suzanne;Stewart, A. Keith;Schimmer, Aaron D.. And the article was included in Blood in 2008.Product Details of 969-33-5 This article mentions the following:

D-cyclins are regulators of cell division that act in a complex with cyclin-dependent kinases to commit cells to a program of DNA replication. D-cyclins are overexpressed in many tumors, including multiple myeloma and leukemia, and contribute to disease progression and chemoresistance. To better understand the role and impact of D-cyclins in hematol. malignancies, we conducted a high throughput screen for inhibitors of the cyclin D2 promoter and identified the drug cyproheptadine. In myeloma and leukemia cells, cyproheptadine decreased expression of cyclins D1, D2, and D3 and arrested these cells in the G₀/G₁ phase. After D-cyclin suppression, cyproheptadine induced apoptosis in myeloma and leukemia cell lines and primary patient samples preferentially over normal hematopoietic cells. In mouse models of myeloma and leukemia, cyproheptadine inhibited tumor growth without significant toxicity. Cyproheptadine-induced apoptosis was preceded by activation of the mitochondrial pathway of caspase activation and was independent of the drug’s known activity as an H1 histamine and serotonin receptor antagonist. Thus, cyproheptadine represents a lead for a novel therapeutic agent for the treatment of malignancy. Because the drug is well tolerated and already approved in multiple countries for clin. use as an antihistamine and appetite stimulant, it could be moved directly into clin. trials for cancer. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Product Details of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Product Details of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Micelle-Enhanced Spectrofluorimetric Method for Determination of Cyproheptadine Hydrochloride in Tablets: Application to In-Vitro Drug Release and Content Uniformity Test was written by Belal, F.;El-Din, M. K. Sharaf;Tolba, M. M.;Elmansi, H.. And the article was included in Journal of Fluorescence in 2014.Related Products of 969-33-5 This article mentions the following:

A highly sensitive and simple spectrofluorimetric method was developed for the determination of cyproheptadine hydrochloride (CYP) in its pharmaceutical formulations. The proposed method is based on the investigation of the fluorescence spectral behavior of CYP in a sodium dodecyl sulfate (SDS) micellar system. In aqueous solution, the fluorescence intensity of CYP was greatly enhanced (150 %) in the presence of SDS. The fluorescence intensity was measured at 410 nm after excitation at 280 nm. The fluorescence-concentration plot was rectilinear over the range 0.2-2.0 渭g/mL, with lower detection limit of 0.06 渭g/mL. The proposed method was successfully applied to the assay of com. tablets as well as content uniformity testing. The application of the proposed method was extended to test the in-vitro drug release of CYP tablets, according to USP guidelines. The results were statistically compared with those obtained by official USP method and were found to be in good agreement. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Related Products of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Related Products of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Determination of cyproheptadine hydrochloride in pure and pharmaceutical forms : a spectrophotometric study was written by Sayanna;Veeraiah, T.;Reddy, Ch. Venkata Ramana. And the article was included in Oriental Journal of Chemistry in 2015.Application of 969-33-5 This article mentions the following:

Siimple and sensitive extractive spectrophotometric methods have been described for the determination of Cyproheptadine hydrochloride (CPH) in pure form and in pharmaceutical formulations. The developed methods involved formation of colored chloroform extractable ion-pair complexes of the CPH with tri-Ph methane dyes viz., bromothymol blue (BTB), bromocresol green (BCG) and bromocresol purple (BCP) in acidic medium. The extracted complexes showed absorbance maxima at 419, 419 and 405nm with use of the above dyes, resp. Beer’s law is obeyed in the concentration ranges 3.0-25, 2.5-22.5 and 1.5-25渭g/mL with BTB, BCG and BCP resp. The stoichiometry of the complex is found to be 1:1 in each case. The effect of concentration of dye, pH and interference of excipients have been studied and optimized. The limit of detection and limit of quantification have been determined for three methods. The methods are applied to the determination of CPH in com. tablets and results of anal. are validated statistically through recovery studies also the methods are validated as per the guidelines of ICH. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Application of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Pre-treatment of BALB/c mice with a centrally acting serotonin antagonist (Cyproheptadine) reduces mortality from Boophone Disticha poisoning was written by Mutseura, M.;Tagwireyi, D.;Gadaga, L. L.. And the article was included in Clinical Toxicology in 2013.Related Products of 969-33-5 This article mentions the following:

Crude extracts of Boophone disticha are used in Southern African traditional medical practice for the management of various illnesses and conditions and have also been abused for their claimed euphoric and hallucinogenic effects. Unfortunately, ingestion of Boophone disticha has resulted in toxicity and death. The results of a recent acute toxicity study in a rat model insinuated that central nervous system (CNS) serotonin overdrive could be the cause of toxicity in B. disticha poisoning. The present work sought to test that hypothesis by investigating whether pre-treatment of B. disticha poisoned BALB/c mice with the CNS acting serotonin antagonist, cyproheptadine, has a dose-dependent protective effect on toxicity and mortality. A hydroethanolic extract of B. disticha was used in all the experiments Five groups each with 10 animals were constituted as follows; a neg. control group (received 10 mL/kg Normal Saline), a pos. control group (received 375 mg/kg of the B. disticha extract), and three test groups each receiving 10 mg/kg, 15 mg/kg and 20 mg/kg cyproheptadine i.p. 15 min before oral gavage administration of 375 mg/kg B. disticha extract resp. The Functional Observational Battery was used to evaluate neurobehavioral and physiol. changes resulting from toxicity of the plant extract The mice were then placed in an open field for another five minutes and the number of rearings and border crossings were counted and recorded. Gait abnormalities, involuntary motor movements, mobility, arousal and stereotypical behavior were also scored according to predefined criteria. All open field investigations were recorded electronically using a LABTEC Webcam and results were later analyzed and recorded by one of the group members. All results were entered on data collection forms. Time to death (survival time) was considered as the time period from dosage with Boophone disticha to time of death. The study follow up period was 7 days and those mice that were alive at the end of the 7 day follow-up period were considered as having survived the poisoning episode. The Kaplan Meier plot and Log-rank test were used to compare differences in mortality and median time to death for mice in the 5 treatment groups. We found that cyproheptadine pre-treatment led to a dose-dependent decrease in mortality from 80% in the group not pre-treated with cyproheptadine, to 30% in the 15 and 20 mg/kg cyproheptadine pre-treated groups (n = 10 per group, p < 0.05). There was also a dose-dependent increase in median survival times amongst the groups (p < 0.0001). Pre-treatment with cyproheptadine also resulted in a decrease of other toxic symptoms associated with Boophone disticha. We conclude that cyproheptadine has a dose-dependent protective effect on mortality and toxicity produced by exposure to Boophone disticha in our mouse model of toxicity. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Related Products of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Related Products of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Cyproheptadine displays preclinical activity in myeloma and leukemia was written by Mao, Xinliang;Liang, Sheng-ben;Hurren, Rose;Gronda, Marcela;Chow, Sue;Xu, G. Wei;Wang, Xiaoming;Zavareh, Reza Beheshti;Jamal, Nazir;Messner, Hans;Hedley, David W.;Datti, Alessandro;Wrana, Jeff L.;Zhu, Yuanxiao;Shi, Chang-xin;Lee, Kyle;Tiedemann, Rodger;Trudel, Suzanne;Stewart, A. Keith;Schimmer, Aaron D.. And the article was included in Blood in 2008.Product Details of 969-33-5 This article mentions the following:

D-cyclins are regulators of cell division that act in a complex with cyclin-dependent kinases to commit cells to a program of DNA replication. D-cyclins are overexpressed in many tumors, including multiple myeloma and leukemia, and contribute to disease progression and chemoresistance. To better understand the role and impact of D-cyclins in hematol. malignancies, we conducted a high throughput screen for inhibitors of the cyclin D2 promoter and identified the drug cyproheptadine. In myeloma and leukemia cells, cyproheptadine decreased expression of cyclins D1, D2, and D3 and arrested these cells in the G₀/G₁ phase. After D-cyclin suppression, cyproheptadine induced apoptosis in myeloma and leukemia cell lines and primary patient samples preferentially over normal hematopoietic cells. In mouse models of myeloma and leukemia, cyproheptadine inhibited tumor growth without significant toxicity. Cyproheptadine-induced apoptosis was preceded by activation of the mitochondrial pathway of caspase activation and was independent of the drug’s known activity as an H1 histamine and serotonin receptor antagonist. Thus, cyproheptadine represents a lead for a novel therapeutic agent for the treatment of malignancy. Because the drug is well tolerated and already approved in multiple countries for clin. use as an antihistamine and appetite stimulant, it could be moved directly into clin. trials for cancer. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Product Details of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Product Details of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Micelle-Enhanced Spectrofluorimetric Method for Determination of Cyproheptadine Hydrochloride in Tablets: Application to In-Vitro Drug Release and Content Uniformity Test was written by Belal, F.;El-Din, M. K. Sharaf;Tolba, M. M.;Elmansi, H.. And the article was included in Journal of Fluorescence in 2014.Related Products of 969-33-5 This article mentions the following:

A highly sensitive and simple spectrofluorimetric method was developed for the determination of cyproheptadine hydrochloride (CYP) in its pharmaceutical formulations. The proposed method is based on the investigation of the fluorescence spectral behavior of CYP in a sodium dodecyl sulfate (SDS) micellar system. In aqueous solution, the fluorescence intensity of CYP was greatly enhanced (150 %) in the presence of SDS. The fluorescence intensity was measured at 410 nm after excitation at 280 nm. The fluorescence-concentration plot was rectilinear over the range 0.2-2.0 μg/mL, with lower detection limit of 0.06 μg/mL. The proposed method was successfully applied to the assay of com. tablets as well as content uniformity testing. The application of the proposed method was extended to test the in-vitro drug release of CYP tablets, according to USP guidelines. The results were statistically compared with those obtained by official USP method and were found to be in good agreement. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Related Products of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Related Products of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Determination of cyproheptadine hydrochloride in pure and pharmaceutical forms : a spectrophotometric study was written by Sayanna;Veeraiah, T.;Reddy, Ch. Venkata Ramana. And the article was included in Oriental Journal of Chemistry in 2015.Application of 969-33-5 This article mentions the following:

Siimple and sensitive extractive spectrophotometric methods have been described for the determination of Cyproheptadine hydrochloride (CPH) in pure form and in pharmaceutical formulations. The developed methods involved formation of colored chloroform extractable ion-pair complexes of the CPH with tri-Ph methane dyes viz., bromothymol blue (BTB), bromocresol green (BCG) and bromocresol purple (BCP) in acidic medium. The extracted complexes showed absorbance maxima at 419, 419 and 405nm with use of the above dyes, resp. Beer’s law is obeyed in the concentration ranges 3.0-25, 2.5-22.5 and 1.5-25μg/mL with BTB, BCG and BCP resp. The stoichiometry of the complex is found to be 1:1 in each case. The effect of concentration of dye, pH and interference of excipients have been studied and optimized. The limit of detection and limit of quantification have been determined for three methods. The methods are applied to the determination of CPH in com. tablets and results of anal. are validated statistically through recovery studies also the methods are validated as per the guidelines of ICH. In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Application of 969-33-5).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application of 969-33-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem