Biomaterial Database

Effects of the alpha 1-adrenoceptor antagonist R-(-)-YM12617 on isolated human penile erectile tissue and vas deferens. 1990

F Holmquist, and H Hedlund, and K E Andersson

Department of Clinical Pharmacology, University Hospital, Lund, Sweden.

The effects of the selective alpha 1-adrenoceptor antagonist, R-(-)-YM12617 (5-[2-[[2-(0-ethoxyphenoxy)ethyl]amino] propyl]-2-methoxybenzenesulphonamide HCl), were investigated in isolated human corpus spongiosum, corpus cavernosum, and vas deferens. R-(-)-YM12617 concentration dependently and competitively inhibited contractions induced by noradrenaline in human penile erectile tissue (pA2 value in corpus spongiosum = 9.92), and the drug was approximately 12 times more potent than prazosin (pA2 value = 8.83). In the vas deferens, R-(-)-YM12617 and prazosin inhibited electrically induced contractions concentration dependently, and abolished the contractions at 10(-6) and 10(-5) M, respectively. The -log IC50 values for R-(-)-YM1261 and prazosin were 8.46 and 7.50, respectively. It is concluded that R-(-)-YM12617 is a potent inhibitor of alpha 1-adrenoceptors in human penile erectile tissues and vas deferens, and that the drug, if injected intracavernosally, may be useful for the treatment of penile erectile dysfunction.

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
D009130	Muscle, Smooth	Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)	Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D009638	Norepinephrine	Precursor of epinephrine that is secreted by the ADRENAL MEDULLA and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers, and of the diffuse projection system in the brain that arises from the LOCUS CERULEUS. It is also found in plants and is used pharmacologically as a sympathomimetic.	Levarterenol,Levonorepinephrine,Noradrenaline,Arterenol,Levonor,Levophed,Levophed Bitartrate,Noradrenaline Bitartrate,Noradrénaline tartrate renaudin,Norepinephrin d-Tartrate (1:1),Norepinephrine Bitartrate,Norepinephrine Hydrochloride,Norepinephrine Hydrochloride, (+)-Isomer,Norepinephrine Hydrochloride, (+,-)-Isomer,Norepinephrine d-Tartrate (1:1),Norepinephrine l-Tartrate (1:1),Norepinephrine l-Tartrate (1:1), (+,-)-Isomer,Norepinephrine l-Tartrate (1:1), Monohydrate,Norepinephrine l-Tartrate (1:1), Monohydrate, (+)-Isomer,Norepinephrine l-Tartrate (1:2),Norepinephrine l-Tartrate, (+)-Isomer,Norepinephrine, (+)-Isomer,Norepinephrine, (+,-)-Isomer
D010410	Penile Erection	The state of the PENIS when the erectile tissue becomes filled or swollen (tumid) with BLOOD and causes the penis to become rigid and elevated. It is a complex process involving CENTRAL NERVOUS SYSTEM; PERIPHERAL NERVOUS SYSTEMS; HORMONES; SMOOTH MUSCLES; and vascular functions.	Tumescence, Penile,Nocturnal Penile Tumescence,Penile Tumescence,Erection, Penile,Penile Tumescence, Nocturnal,Tumescence, Nocturnal Penile
D010413	Penis	The external reproductive organ of males. It is composed of a mass of erectile tissue enclosed in three cylindrical fibrous compartments. Two of the three compartments, the corpus cavernosa, are placed side-by-side along the upper part of the organ. The third compartment below, the corpus spongiosum, houses the urethra.	Glans Penis,Penis, Glans
D011224	Prazosin	A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.	Furazosin,Minipress,Pratsiol,Prazosin HCL,Prazosin Hydrochloride,HCL, Prazosin,Hydrochloride, Prazosin
D004558	Electric Stimulation	Use of electric potential or currents to elicit biological responses.	Stimulation, Electric,Electrical Stimulation,Electric Stimulations,Electrical Stimulations,Stimulation, Electrical,Stimulations, Electric,Stimulations, Electrical
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man