Functional characterization of alpha-1-adrenoceptor subtypes in the prostatic urethra and trigone of male rabbit. 1996

V Deplanne, and A M Galzin
Synthélabo Recherche (L.E.R.S.), Cardiovascular Department, Bagneux, France.

The effects of alpha-1-adrenoceptor antagonists on the concentration-response curves (CRC) to phenylephrine and oxymetazoline have been studied in prostatic urethra and trigone of male adult rabbits (28 wk old). WB4101 and phentolamine, at low concentrations which should preferentially antagonize the alpha-1A-adrenoceptor subtype, did not modify the oxymetazoline-induced contraction of both prostatic urethra and trigone, suggesting that alpha-1A-adrenoceptors are not activated under these conditions. In urethra, pretreatment with 50 microM chloroethylclonidine (CEC), significantly reduced the maximal contraction to both agonists to 60 and 70% of control, respectively. In trigone, CEC decreased the maximum contraction to phenylephrine, but not to oxymetazoline, by 50%. In addition, CEC shifted to the right the CRC to both agonists. These results suggest the presence of an alpha-1B-adrenoceptor in both rabbit urethra and trigone. Exposure to prazosin (0.01-1 microM) significantly shifted to the right the CRC to phenylephrine (pA2 or affinity values without CEC treatment: 7.77 and 7.96 in urethra and trigone respectively; with CEC pretreatment: 7.49 and 7.42, respectively). When oxymetazoline was used as an agonist and in the presence of CEC, prazosin was unexpectedly weak in urethra with an affinity value of 6.70, although the antagonist potency was not modified in trigone (affinity 7.38). These values suggest that alpha-1-adrenoceptor agonists contract rabbit urethra and trigone through activation of alpha-1-adrenoceptors displaying low affinity for prazosin. Whether this receptor coincides with the alpha-1L- or alpha-1N-subtype remains to be clarified.

UI MeSH Term Description Entries
D008297 Male Males
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
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
D010109 Oxymetazoline A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251) Oxymetazoline Hydrochloride,Hydrochloride, Oxymetazoline
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
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
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
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
D000322 Adrenergic Agonists Drugs that bind to and activate adrenergic receptors. Adrenomimetics,Adrenergic Agonist,Adrenergic Receptor Agonist,Adrenergic Receptor Agonists,Receptor Agonists, Adrenergic,Agonist, Adrenergic,Agonist, Adrenergic Receptor,Agonists, Adrenergic,Agonists, Adrenergic Receptor,Receptor Agonist, Adrenergic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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