Abstract:
:The effects of acute or repeated treatment of male albino BKW mice with caerulein, a cholecystokinin octapeptide (CCK-8) agonist, and with devazepide (MK-329) and L-365,260, antagonists at CCKA ('peripheral') and CCKB ('central') receptors respectively, on motor activity and [propionyl-3H]propionylated-CCK-8 ([3H]pCCK-8) binding were studied. Acute treatment with a large dose of caerulein (100 micrograms/kg s.c.) suppressed motor activity (line crossings and rearings) whereas devazepide (2 mg/kg i.p.) had the opposite action. L-365,260 (2 mg/kg i.p.) increased only the number of rearings. Tolerance developed to the locomotor effects of caerulein and devazepide when these same doses were administered once daily (caerulein) or twice daily (devazepide) for 10 days. Twice daily administration of L-365,260 (2 mg/kg) for 10 days did not significantly alter the locomotor activity of mice. The sedative effect of caerulein (20 micrograms/kg s.c.) was markedly reduced in mice receiving repeated injections of either a larger amount of caerulein (100 micrograms/kg) or devazepide but not after L-365,260. The stimulant effect of (+)-amphetamine (2 mg/kg s.c.) on motor activity was increased by subchronic administration of either devazepide or caerulein, but not by L-365,260. All three compounds (caerulein, devazepide and L-365,260) increased the number of [( 3H]pCCK-8 binding sites in mouse forebrain but the increase was only significant after L-365,260. The effects of long-term treatment with caerulein are probably related to the stimulation of CCKA receptors, whereas the paradoxically similar action of devazepide may be linked to the blockade of both subtypes of the CCK-8 receptor.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Vasar E,Stephenson JD,Meldrum BSdoi
10.1016/0014-2999(91)90283-vsubject
Has Abstractpub_date
1991-09-24 00:00:00pages
385-90issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(91)90283-Vjournal_volume
202pub_type
杂志文章abstract::The prostaglandin synthetase inhibitors indomethacin and acetyl salicylic acid did not affect the post-stimulus rebound excitation of guinea-pig duodenal and jejunal circular muscle with transmural electrical stimulation at 1 min intervals. In the absence of any drug, sequential time-dependent changes in amplitude of ...
journal_title:European journal of pharmacology
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doi:10.1016/0014-2999(76)90354-x
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journal_title:European journal of pharmacology
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