Library

feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    ISSN: 1432-1912
    Keywords: Vasopressin release ; Oxytocin release ; Neurohypophysis ; Potassium channels ; Stimulus secretion coupling ; Tetraethylammonium ions ; Aminopyridines
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Isolated rat neurohypophyses were fixed by their stalks to a platinum wire electrode and superfused with Krebs-HEPES solution. Vasopressin and oxytocin released into the medium were determined by specific radioimmunoassays. Hormone secretion was increased by electrical stimulation of the pituitary stalk at different frequencies. The effects of several potassium channel blockers, tetraethylammonium (TEA) ions, 4-aminopyridine (4-AP) and 3,4-diaminopyridine (3,4-DAP) were tested. The release of vasopressin and oxytocin evoked by electrical stimulation with 900 pulses at 15 Hz (about 900 and 1,000 μU, respectively) was about 10 times higher than that evoked by 900 pulses at 3 Hz. Both 10 and 30 mmol/l TEA enhanced the release of vasopressin evoked by stimulation at 3 and 15 Hz, by 25- and 2-fold, respectively, to attain a maximum release of about 1,800 μU per stimulation. The stimulated release of oxytocin attained a maximum of about 9,000 μU at 15 Hz in the presence of 10 mmol/l TEA or at 3 Hz with 30 mmol/l TEA. Thus, in the presence of maximally effective concentrations of TEA both stimulation frequencies (3 and 15 Hz) were equieffective in evoking release of vasopressin and oxytocin. 4-AP or 3,4-DAP enhanced the release of vasopressin evoked by 15 Hz stimulation maximally to about 1,600 μU and that evoked by 3 Hz stimulation to about 900 μU. In the presence of 4-AP or 3,4-DAP the release of oxytocin evoked by stimulation at 15 Hz increased maximally to about 8,000 μU and that evoked by stimulation at 3 Hz to about 1,500 μU. Thus, in the presence of maximally effective concentrations of 4-AP or 3,4-DAP stimulation at 15 Hz induced a significantly higher release of vasopressin and oxytocin than stimulation at 3 Hz. Naloxone (1 μmol/l) increased the release of oxytocin evoked by stimulation at 15 Hz to about 3,000 μU and that evoked by stimulation at 3 Hz to about 700 μU. The release of oxytocin evoked by stimulation at 15 Hz in the presence of 10 mmol/l TEA or 1 mmol/l 4-AP (about 8,000–9,000 μU) was not further enhanced by naloxone. However, during stimulation at 1 or 3 Hz in the presence of 10 mmol/l TEA, naloxone increased the release of oxytocin from about 3,700 and 6,300 μU, respectively, to the maximum of about 9,000 μU. Likewise, during stimulation at 3 Hz in the presence of 1 mmol/14-AP, naloxone increased the relase of oxytocin from about 1,500 to 9,000 μU. Under all condition studied, naloxone did not affect the release of vasopressin. In conclusion, neurosecretory nerve endings are endowed with different types of potassium channels. Blockade of potassium channels can oppose the opioid inhibition of oxytocin release in a complex frequency-dependent manner.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    ISSN: 1432-1912
    Keywords: Rabbit perfused atria ; [14C]Acetylcholine release ; Noradrenaline release ; Presynaptic M1 receptor ; Cholinergic-adrenergic interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Rabbit atria were isolated with the extrinsic right vagus and sympathetic nerves intact and perfused with Tyrode solution. Noradrenaline overflow evoked by sympathetic nerve stimulation (SNS) at 3 Hz for 3 min was determined before, during, and after vagus nerve stimulation (VNS), also at 3 Hz and for 3 min. The VNS pulses preceded the SNS pulses by 3, 100 and 233 ms. Acetylcholine overflow was determined after labelling of the transmitter stores with [14C]choline. Pirenzepine 80 nmol/l failed to alter the muscarinic inhibition of noradrenaline overflow when the vago-sympathetic impulse intervals were 3 and 233 ms. At an interval of 100 ms VNS did not significantly inhibit noradrenaline overflow in the absence of pirenzepine but produced an inhibition in the presence of the drug. When the pirenzepine concentration was varied (0.4–300 nmol/l) the largest inhibition of noradrenaline overflow was observed at 5.7 nmol/l whereas 300 nmol/l fully antagonized the inhibition. Acetylcholine overflow evoked by VNS was not altered by pirenzepine 0.4–300 nmol/l. AF-DX 116 (11-[{2[oi(diethylamino)methyl]-1-piperidinyl}-acetyl]-5,11-dihydro-6H-pyrido-[2,3-b]-[1,4]benzodiazepine-6-one), an M2 receptor selective antagonist, concentration-dependently (100–800 nmol/l) inhibited the decrease of tension development elicited by VNS. At the 100 ms vago-sympathetic impulse interval noradrenaline overflow was enhanced in the presence of AF-DX 116 400 and 800 nmol/l. However, already 100 nmol/l of the drug caused a maximum (fourfold) increase of acetylcholine overflow. It is concluded that acetylcholine released onto noradrenergic nerve fibres causes a small facilitation of noradrenaline overflow at a vago-sympathetic impulse interval of 100 ms. This response is mediated by an M1 receptor and is superimposed on the well-known M2 receptor mediated inhibition of noradrenaline release which is obtained at vago-sympathetic impulse intervals ranging between 3 and 233 ms. The M2 autoreceptor regulating acetylcholine release is activated by lower synaptic concentrations of the transmitter than the M2 heteroreceptor regulating noradrenaline release.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 345 (1992), S. 611-618 
    ISSN: 1432-1912
    Keywords: Muscarinic receptor subtypes ; Rabbit iris sphincter muscle ; Guinea-pig uterus ; Rat iris ; Preand postjunctional dissociation constants
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In order to analyse the subtype of muscarinic receptors involved in the methacholine-induced contraction of the rabbit iris sphincter we have determined equilibrium dissociation constants (KB) of various antagonists in the sphincter muscle. The values were compared with those observed at M1 (rabbit vas deferens), M2 (heteroreceptors in rat iris) and M3 receptors (guinea-pig ileum), or at the muscarinic receptors in the guinea-pig uterus. The methacholine-induced contraction of the uterus from immature guinea-pigs was competitively antagonized by pirenzepine (6.64, −log KB), 4-DAMP (8.39), hexahydrodifenidol (HHD; 7.00 for the (R)- and 5.40 for the (S)-enantiomer), p-fluoro-hexahydrosiladifenidol (pF-HHSiD; 6.25) and valethamate bromide (8.04). The affinity of the antagonists is consistent with the presence of an M2 receptor. The −log KB values of the antagonists in the rabbit iris sphincter (6.43, p-F-HHSiD; 6.22, AQ-RA 741; 7.23 and 5.34, (R)- and (S)-trihexyphenidyl) were lower than, or within the lowest range of, estimates in the other experimental models, irrespective of the subtype selectivity of the antagonist. This excludes the presence of an M1, M2, M3 or M4 receptor in this smooth muscle. The affinity of UH-AH 37 in the iris was intermediate between that for M1 or M3, and M2 receptors. The low affinity of AQRA 741 and the low enantiomeric ratio of trihexyphenidyl (THP) in the iris (77.6) would be compatible with a presumed M5 receptor. Valethamate bromide and clozapine did not differentiate between M1, M2 and M3 receptors in the present functional studies; the pA2 values at the M1–M3 sites (8.46–8.57 and 7.26–7.58, respectively) were about 10 and 100 times higher, respectively, than the estimates in the iris sphincter. In absolute terms, however, our −log KB values of the THP-enantiomers, UH-AH 37 and clozapine in the iris sphincter were 0.8–2 log units lower than previous data on cloned m5 receptors suggesting receptor properties different from the presumed M5 receptor. In conclusion, the muscarinic receptors in the rabbit iris sphincter may represent a novel type differing from M1–M4 receptors.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...