Identification of α1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens

Buccioni, Michela; Kandhavelu, Meenakshisundaram; Angeli, Piero; Cristalli, Gloria; Ben, Diego Dal; Giardinà, Dario; Lambertucci, Catia; Lammi, C.; Volpini, Rosaria; Marucci, Gabriella

doi:10.1016/j.ejphar.2008.10.067

Cited by 9 publications

(7 citation statements)

References 26 publications

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“…It has been variously suggested that contractions of rat vas deferens to exogenous noradrenaline or adrenaline are mediated predominantly by α 1A ‐adrenoceptors (Han et al ., ; Hanft & Gross, ; Aboud et al ., ; Teng et al ., ; Burt et al ., ; Buckner et al ., ; Honner & Docherty, ), α 1D ‐ in addition to α 1A ‐adrenoceptors (Cleary et al ., ) or α 1L ‐ in addition to α 1A ‐adrenoceptors (Ohmura et al ., ; Buccioni et al ., ). A wide range of prazosin pA 2 values has been reported in rat vas deferens: 8.32–8.39 (Ohmura et al ., ), 8.59–9.34 (Honner & Docherty, ), 9.20 (Burt et al ., ), 9.26 (Aboud et al ., ), 9.30 (Amobi et al ., ) and 9.35 (Lima et al ., ).…”

Section: Introductionmentioning

confidence: 99%

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens

Docherty¹

2013

Auton Autocoid Pharmacol

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(1) We have investigated α1 -adrenoceptor subtypes mediating contractions to noradrenaline in epididymal portions of rat vas deferens. (2) Contractions to noradrenaline were investigated in the absence or presence of the noradrenaline transporter blocker cocaine. (3) In the absence of cocaine, contractions to noradrenaline were potently antagonized by RS100329, but not by BMY7378, and so are mediated mainly by α1A -adrenoceptors. (4) In the presence of cocaine, noradrenaline potency was increased, particularly in terms of low concentrations and phasic contractions. Contractions to low concentrations of noradrenaline in the presence of cocaine were resistant to RS100329 but potently antagonized by BMY7378, demonstrating that α1D-adrenoceptors are additionally involved in contractions amplified by cocaine. (5) In the absence of cocaine, prazosin exhibited relatively low potency as an antagonist against the α1A-adrenoceptor-mediated component to the response. In the presence of cocaine, prazosin exhibited higher potency against the α1D-adrenoceptor-mediated component. (6) In conclusion, prazosin has previously unreported selectivity for α1D-over α1A -adrenoceptors in functional studies of rat vas deferens. Contractions of rat vas deferens are mediated by α1A-and α1D -adrenoceptors. The range of prazosin potencies and of receptor subtypes previously reported in rat vas deferens may be explained by the presence of these two subtypes.

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Section: Introductionmentioning

confidence: 99%

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens

Docherty¹

2013

Auton Autocoid Pharmacol

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“…This tissue was used to assess α 1A -AR antagonism [38]. Prostatic portions of 2-cm length were mounted under 0.35 g tension at 37 °C in a Tyrode solution of the following composition (mM):…”

Section: Rat Vas Deferens Prostatic Portionmentioning

confidence: 99%

High affinity ligands and potent antagonists for the α1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives

Romeo

Salerno

Pittalà

et al. 2014

European Journal of Medicinal Chemistry

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“…The isolated rat vas deferens is valuable for characterization of α 1A -adrenoceptor responses (see Basic Protocol 1 and Table 4.5.1). There is considerable literature on the use of rat vas deferens for this purpose, including studies demonstrating this tissue is enriched in α 1A -adrenoceptor sites (Furukawa et al, 1995;Noble et al, 1995, Buccioni et al, 2009.…”

Section: α 1 -Adrenoceptorsmentioning

confidence: 99%

α‐Adrenoceptor Assays

Abel

Jain

2012

CP Pharmacology

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α-Adrenoceptors mediate responses to activation of both peripheral sympathetic nerves and central noradrenergic neurons. They also serve as autoreceptors that modulate the release of norepinephrine (NE) and other neurotransmitters. There are two major classes of α-adrenoceptors, the α(1)- and α(2). Each class is subdivided into three subtypes: α(1A), α(1B), α(1D), and α(2A), α(2B), α(2C). Described in this unit are in vitro isolated tissue methods used to study α-adrenoceptor functions and to identify novel ligands for these receptors. Detailed protocols describing use of isolated tissues to study the various α(1)- and α(2)-adrenoceptor subtypes are provided.

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Identification of α1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens

Cited by 9 publications

References 26 publications

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens

High affinity ligands and potent antagonists for the α1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives

α‐Adrenoceptor Assays

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Identification of α1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens

Cited by 9 publications

References 26 publications

Prazosin has low potency at α1A‐adrenoceptors and high potency at α1D‐adrenoceptors in rat vas deferens

Prazosin has low potency at α1A‐adrenoceptors and high potency at α1D‐adrenoceptors in rat vas deferens

High affinity ligands and potent antagonists for the α1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives

α‐Adrenoceptor Assays

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Product

Resources

About

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens

Prazosin has low potency at α_1A‐adrenoceptors and high potency at α_1D‐adrenoceptors in rat vas deferens