Metabolic fate of the new .BETA.-adrenoceptor antagonist, bisoprolol, in animals (3): Foeto-placental transfer and excretion into milk of 14C-bisoprolol in rats.

1989 ◽  
Vol 4 (2) ◽  
pp. 173-185
Author(s):  
Yasuhiro YAMADA ◽  
Mika NAKAHARA ◽  
Kazuaki NAITO ◽  
Michihiro KOHNO ◽  
Minezo OTSUKA ◽  
...  
Keyword(s):  
Placental Transfer ◽  
Metabolic Fate ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist

scholarly journals Metabolic fate of the new .BETA.-adrenoceptor antagonist, bisoprolol, in animals (1): Absorption, distribution and excretion of 14C-bisoprolol in rats.

1989 ◽  
Vol 4 (2) ◽  
pp. 149-164
Author(s):  
Yasuhiro YAMADA ◽  
Mika NAKAHARA ◽  
Kazuaki NAITO ◽  
Michihiro KOHNO ◽  
Minezo OTSUKA ◽  
...  
Keyword(s):  
Metabolic Fate ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist

scholarly journals Metabolic fate of the new .BETA.-adrenoceptor antagonist, bisoprolol, in animals (2): Tissue accumulation after consecutive oral administration of 14C-bisoprolol in rats.

1989 ◽  
Vol 4 (2) ◽  
pp. 165-172
Author(s):  
Yasuhiro YAMADA ◽  
Mika NAKAHARA ◽  
Kazuaki NAITO ◽  
Michihiro KOHNO ◽  
Minezo OTSUKA ◽  
...  
Keyword(s):  
Oral Administration ◽  
Metabolic Fate ◽  
Tissue Accumulation ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist

scholarly journals Pharmacokinetics, pharmacodynamics, and safety of bevantolol, a new .BETA.1-selective .BETA.-adrenoceptor antagonist, in Japanese healthy volunteers.

1989 ◽  
Vol 20 (3) ◽  
pp. 551-564
Author(s):  
Kouichi SUGIMOTO ◽  
Akio EBIHARA ◽  
Akio FUJIMURA ◽  
Hisatoshi ORIBE ◽  
Naoko HINO ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist

Actions of norepinephrine on rat hypoglossal motoneurons

1995 ◽  
Vol 74 (5) ◽  
pp. 1911-1919 ◽  
Author(s):  
M. A. Parkis ◽  
D. A. Bayliss ◽  
A. J. Berger
Keyword(s):  
Choline Chloride ◽  
Reversal Potential ◽  
Repetitive Firing ◽  
Inward Current ◽  
Hypoglossal Motoneurons ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist ◽  
Perfusion Solution ◽  
Adrenoceptor Agonist ◽  
Firing Properties

1. We used conventional intracellular recording techniques in 400-microns-thick slices from the brain stems of juvenile rats to investigate the action of norepinephrine (NE) on subthreshold and firing properties of hypoglossal motoneurons (HMs). 2. In recordings in current-clamp mode, 50 or 100 microM NE elicited a reversible depolarization accompanied by an increase in input resistance (RN) in all HMs tested (n = 74). In recordings in single-electrode voltage-clamp mode, NE induced a reversible inward current (INE) accompanied by a reduction in input conductance. The average reversal potential for INE was -104 mV. The NE responses could be elicited in a Ca(2+)-free solution containing tetrodotoxin, indicating that they were postsynaptic. 3. The NE response could be blocked by the alpha-adrenoceptor antagonist prazosin, but not by the beta-adrenoceptor antagonist propranolol, and could be mimicked by the alpha 1-adrenoceptor agonist phenylephrine but not by the alpha 2-adrenoceptor agonist UK 14,304 or by the beta-adrenoceptor agonist isoproterenol when alpha-adrenoceptors were blocked. 4. Substitution of barium for calcium in the perfusion solution blocked the increase in RN in response to NE without completely blocking the depolarization. Replacement of sodium chloride with choline chloride in the barium-substituted perfusion solution blocked the remaining depolarization. 5. The neuropeptide thyrotropin-releasing hormone (TRH), which also depolarizes and increases the RN of HMs, occluded the response of HMs to NE. 6. NE altered HM firing properties in three ways: it always lowered the minimum amount of injected current needed to elicit repetitive firing, it increased the slope of the firing frequency versus injected current relation in 8 of 14 cells tested, and it increased the delay from the onset of the depolarizing current pulse to the first evoked spike in all cells tested. 7. We conclude that NE acts directly on alpha 1-adrenoceptors to increase the excitability of HMs. It does this by reducing a barium-sensitive resting potassium current and activating a barium-insensitive inward current carried primarily by sodium ions. A portion of the intracellular pathway for these actions is shared by TRH. In addition, there is evidence that NE alters HM firing patterns by affecting currents that are activated following depolarization.

scholarly journals Studies on Metabolic Fate of 14C-RU44570: Placental Transfer, Transfer into Milk, Absorption Site and Repeated Dosing in Rats, and Metabolism in Rats and Dogs.

1994 ◽  
Vol 9 (6) ◽  
pp. 762-792
Author(s):  
Masashi HIRAYAMA ◽  
Tatsuo MANABE ◽  
Yoshinari HASEGAWA ◽  
Yoshiharu KATAMI ◽  
Katsumi UOHAMA ◽  
...  
Keyword(s):  
Placental Transfer ◽  
Metabolic Fate ◽  
Repeated Dosing

scholarly journals Metabolic Fate of NKH477. (3). Feto-Placental Transfer and Excretion into Milk in Rats after a Single Intravenous Administration.

1998 ◽  
Vol 13 (3) ◽  
pp. 229-236
Author(s):  
Tsuyoshi IRIE ◽  
Shin-ichi MATSUMOTO ◽  
Rika GODA ◽  
Toshiko EKI ◽  
Kouwa YAMASHITA
Keyword(s):  
Intravenous Administration ◽  
Placental Transfer ◽  
Metabolic Fate ◽  
Single Intravenous Administration

Beta adrenoceptors mediate the catecholamine-induced stimulation of oxytocin secretion from cultured bovine granulosa cells

1991 ◽  
Vol 3 (6) ◽  
pp. 715 ◽  
Author(s):  
MR Luck ◽  
M Munker
Keyword(s):  
Granulosa Cells ◽  
Receptor Subtype ◽  
Alpha Adrenoceptors ◽  
Beta Adrenoceptor ◽  
Adrenoceptor Antagonist ◽  
Adrenoceptor Agonist ◽  
Ici 118,551 ◽  
Beta 2 ◽  
Term Response

Bovine granulosa cells were treated in culture with alpha- and beta-adrenoceptor ligands to determine the receptor subtype mediating their response to catecholamines. The secretion of oxytocin by granulosa cells in serum-free medium was measured on the fourth day of culture (during the period of acquisition of a luteal phenotype). Cultures were performed in the presence of 0.5 mM ascorbic acid, which increased hormone output and potentiated the response to catecholamines. The effects of adrenaline and noradrenaline on oxytocin secretion were concentration-dependent; maximum stimulation was over 700% with adrenalin (EC50 92 nM) and 500% with noradrenaline (EC50 87 nM). The response to noradrenaline (10(-6) M) and adrenaline (10(-6) M) could be blocked by propranolol but not by phentolamine, suggesting that beta- rather than alpha-adrenoceptors were involved. Blockade by metoprolol and practolol (beta 1-adrenoceptor antagonists) was poor and dobutamine (beta 1-agonist) was weakly stimulatory. A concentration-dependent stimulatory response (EC50 200 nM) was obtained with salbutamol (beta 2-adrenoceptor agonist) and stimulation by adrenaline or salbutamol could be blocked by a selective beta 2-adrenoceptor antagonist (ICI 118,551). It is concluded that, during luteinization, the long-term response of bovine granulosa cells to stimulation induced by catecholamines is mediated through beta- rather than alpha-adrenoceptors. Although the beta 2-subtype is probably involved, the similar potencies of adrenaline and noradrenaline are uncharacteristic of beta 2-adrenoceptors and may be peculiar to the long-term response shown by these cells.

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