Physiological and pharmacological aspects of adrenergic receptor classification

Ariëns, E. J.; Simonis, A. M.

doi:10.1016/0006-2952(83)90324-6

Cited by 127 publications

(37 citation statements)

References 39 publications

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“…on classical hormone receptors, and noradrenaline is believed to act on ß,-receptors, i.e. on neural receptors (Ariens & Simonis, 1983), our findings indicate that circulating adrenaline can act as a physiological hormone in rat corpora lutea.…”

Section: Discussionsupporting

confidence: 49%

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

Norjavaara

Rosberg²,

Gåfvels³

et al. 1989

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Summary. Luteal \g=b\-adrenergicreceptor concentration and subtype were determined in adult pseudopregnant rats during and after the period of the functional luteal phase.was used to determine the receptor concentration in corpora lutea of adult pseudopregnant rats. A 3-fold increase in \g=b\-adrenergicreceptor concentration was seen during the first 2\p=n-\3 days of pseudopregnancy, whereafter the receptor concentration declined. During the functional luteal regression period (Day 12\p=n-\15) the receptor levels were still low. In regressed (Day 16\p=n-\22)corpora lutea a temporary increase in \g=b\-receptor concentration was seen which may represent some role for \g=b\-adrenergic mechanisms in the regulation of morphological regression in the corpus luteum.To determine the \g=b\-adrenergicsubtype, competition of [125I]ICYP-binding with selective \ g=b\ 1 and \g=b\2-adrenergic antagonists was assessed in corpora lutea of different ages and in rat heart and uterus. The \g=b\-adrenergicreceptors in corpora lutea of adult pseudopregnant rats were shown to be solely of the subtype \ g=b\ 2, regardless of the luteal age.

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Section: Discussionsupporting

confidence: 49%

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

Norjavaara

Rosberg²,

Gåfvels³

et al. 1989

Reproduction

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“…One of the reasons for comparing the effects of metoprolol and propranolol in the present study was to evaluate the importance of adrenaline, since adrenaline is 032-selective when acting as a circulating hormone (Ariens & Simonis, 1983;Hjemdahl et al, 1983). The present study showed no differences between the two 1-adrenoceptor antagonists with regard to circulatory responses.…”

Section: Discussionmentioning

confidence: 99%

Responses to mental stress and physical provocations before and during long term treatment of hypertensive patients with beta‐adrenoceptor blockers or hydrochlorothiazide.

Eliasson

Kahan

Hylander

et al. 1987

Brit J Clinical Pharma

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1 Cardiovascular and sympatho-adrenal responsiveness to mental stress (CWT; a colour word test), orthostatic testing (ORT) and a cold pressor test (CPT) were examined in three groups of hypertensive patients (n = 14-16) before and after 6 months treatment with metoprolol (243 ± 26 mg daily), propranolol (149 ± 16 mg daily) or hydrochlorothiazide (50 ± 8 mg daily) in an open trial design. 2 Treatment reduced outpatient blood pressures in the three groups similarly (from approximately 155/102 to 135/90 mm Hg). During treatment resting blood pressures in the laboratory were clearly reduced by P-adrenoceptor blockade but not by thiazide treatment. Metoprolol and propranolol caused similar reductions of basal heart rates and plasma glycerol levels, whereas only propranolol reduced cyclic AMP concentrations in plasma. 3 Before treatment CWT and CPT increased systolic and diastolic blood pressures by about 30%. Heart rate increased by about 30 beats min-' during CWT and 10-15 beats min-' during CPT and ORT. Small venous plasma adrenaline responses were evoked by all tests, whereas noradrenaline was elevated mainly by CPT and ORT. Dopamine levels did not change. 4 Heart rate responses to all stressors were markedly and similarly reduced, whereas blood pressure responses were essentially unchanged during metoprolol or propranolol treatment. In the thiazide group circulatory responses to CWT were slightly attenuated, whereas responses to ORT and CPT were unchanged. 5 The systolic blood pressure levels were reduced throughout the test session in all three groups, although less so in the hydrochlorothiazide group. Both 3-adrenoceptor antagonists clearly reduced diastolic blood pressure and heart rate levels at rest and during stress, whereas thiazide treatment caused no significant changes in these respects. 6 The rate pressure product, which increased by 80-100% in response to CWT before treatment, was more markedly reduced by 3-adrenoceptor blockade than by thiazide treatment both at rest and during stress.7 Self ratings (visual analogue scales) of stress and irritation were increased by CWT in a similar fashion before and during treatment in all groups. ,B-adrenoceptor blockade was associated with higher subjective ratings of tiredness at rest, but not after CWT. Perfor-

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“…However, one potential problem of using antagonist radioligands is that they may not identify the precise site at which the endogenous neurotransmitter acts. It has been pointed out that agonists are small molecules relatively rich in polar groups whereas antagonists tend to be larger and composed of a hydrophobic centre and a smaller polar group (Ariens & Simonis, 1983). The characteristics of antagonists therefore tend to favour binding to lipophilic sites which are close to the polar sites acted on by the agonists.…”

Section: Discussionmentioning

confidence: 99%

[³H]‐rauwolscine binding to α₂‐adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species

Neylon

Summers

1985

British J Pharmacology

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(2.33-3.03 nM) except man where it was significantly higher (0.98 nM). Marked differences were seen in the density of binding sites, increasing in the order: man < dog < rabbit < rat < mouse. In all cases, Hill coefficients were not significantly different from unity. 4 [3H]-rauwolscine binds with low affinity (KD> 15 nM) to membranes prepared from guinea-pig kidney. The low affinity binding is not due to the absence of particular ions in the incubation medium or to receptor occupation by endogenous agonist. 5 The binding in all species was found to be stereoselective with respect to the isomers of noradrenaline. However, differences were seen in the characteristics of agonist interactions with the binding site both between isomers and between species.6 Marked differences in affinity of particular a-adrenoceptor antagonists were observed for a2-adrenoceptors labelled by [3H]-rauwolscine. These differences were most evident with the a,-adrenoceptor selective antagonist prazosin which displayed inhibition constants (K, values) of 33.2, 39.5, 261, 570 and 595 nM in rat, mouse, dog, man and rabbit, respectively. 7 Differences are apparent in the characteristics of a2-adrenoceptors labelled by [3H]-rauwolscine between species and it is suggested that the differences observed for a,-selective antagonists such as prazosin may be related to binding to additional sites in the vicinity of the a2-adrenoceptor.

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Physiological and pharmacological aspects of adrenergic receptor classification

Cited by 127 publications

References 39 publications

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

Responses to mental stress and physical provocations before and during long term treatment of hypertensive patients with beta‐adrenoceptor blockers or hydrochlorothiazide.

[³H]‐rauwolscine binding to α₂‐adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species

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Physiological and pharmacological aspects of adrenergic receptor classification

Cited by 127 publications

References 39 publications

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

-Adrenergic receptor concentration and subtype in the corpus luteum of the adult pseudopregnant rat

Responses to mental stress and physical provocations before and during long term treatment of hypertensive patients with beta‐adrenoceptor blockers or hydrochlorothiazide.

[3H]‐rauwolscine binding to α2‐adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species

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[³H]‐rauwolscine binding to α₂‐adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species