Biomaterial Database

Investigation of the effects of some alkaloidal alpha1-adrenoceptor antagonists on human hyperplastic prostate. 1999

J H Guh, and C H Hsieh, and C M Teng

Pharmacological Institute, College of Medicine, National Taiwan University, Taipei.

The effects of N-allylsecoboldine, (-)-discretamine, ( )-govadine and [(+/-)-2,3,10,11-tetrahydroxytetrahydroproto-berberine HBr] ((+/-)-THP) on contractile responses were investigated in human hyperplastic prostate. They all inhibited, concentration dependently, the tension responses to phenylephrine and electrical field stimulation, and the pA2 and pIC50 values were calculated. The relative potencies of these four agents with reference to prazosin were obtained. The results showed that N-allylsecoboldine exhibited greater potency (4.1-fold), whereas (-)-discretamine, (+/-)-govadine and (+/-)-THP had similar potencies, against contractions elicited by electrical field stimulation and against contractions elicited by phenylephrine in human hyperplastic prostate. In addition, the potency ratios of N-allylsecoboldine, (-)-discretamine, (+/-)-govadine and (+/-)-THP against phenylephrine-induced contractions in rat vas deferens/spleen were 7.78, 0.89, 0.57, and 0.96, respectively. In the presence of prazosin (0.3 +/-M) to block alpha1-adrenoceptor-mediated responses, nifedipine (10 microM), but not the above four agents, significantly blocked KCl (60 mM)-induced tension responses in human hyperplastic prostate. It is suggested that N-allylsecoboldine exhibits greater potency against nerve-mediated contraction than against phenylephrine-induced contraction in human hyperplastic prostate and that this antagonistic effect is due mainly to its high affinity for the alpha1A-adrenoceptor subtype.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D008875	Middle Aged	An adult aged 45 - 64 years.	Middle Age
D009119	Muscle Contraction	A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009543	Nifedipine	A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.	Adalat,BAY-a-1040,Bay-1040,Cordipin,Cordipine,Corinfar,Fenigidin,Korinfar,Nifangin,Nifedipine Monohydrochloride,Nifedipine-GTIS,Procardia,Procardia XL,Vascard,BAY a 1040,BAYa1040,Bay 1040,Bay1040,Monohydrochloride, Nifedipine,Nifedipine GTIS
D010656	Phenylephrine	An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.	(R)-3-Hydroxy-alpha-((methylamino)methyl)benzenemethanol,Metaoxedrin,Metasympatol,Mezaton,Neo-Synephrine,Neosynephrine,Phenylephrine Hydrochloride,Phenylephrine Tannate,Neo Synephrine,Tannate, Phenylephrine
D011188	Potassium	An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
D011467	Prostate	A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM.	Prostates
D011470	Prostatic Hyperplasia	Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.	Adenoma, Prostatic,Benign Prostatic Hyperplasia,Prostatic Adenoma,Prostatic Hyperplasia, Benign,Prostatic Hypertrophy,Prostatic Hypertrophy, Benign,Adenomas, Prostatic,Benign Prostatic Hyperplasias,Benign Prostatic Hypertrophy,Hyperplasia, Benign Prostatic,Hyperplasia, Prostatic,Hyperplasias, Benign Prostatic,Hypertrophies, Prostatic,Hypertrophy, Benign Prostatic,Hypertrophy, Prostatic,Prostatic Adenomas,Prostatic Hyperplasias, Benign,Prostatic Hypertrophies
D002118	Calcium	A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.	Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response