Abstract：
:We have investigated the effects of antagonists at functional prejunctional alpha 2-adrenoceptors of rat was deferens and rat submandibular gland and compared potencies with affinities for the alpha 2A-, alpha 2B- and putative alpha 2D-ligand binding sites of human platelet, rat kidney, and rat submandibular gland, respectively. Prejunctional potency of antagonists was expressed as an EC30 (concentration producing a 30% increase in stimulation-evoked release of tritium in tissues pre-incubated with [3H]noradrenaline) in rat vas deferens and submandibular gland, and also as a pA2 (antagonist concentration producing a 2-fold shift in the inhibition by the alpha 2-adrenoceptor agonist xylazine of the electrically-evoked isometric twitch) in rat vas deferens. The functional prejunctional alpha 2-adrenoceptors of rat vas deferens and submandibular gland are alpha 2A-like since there was a good correlation between affinity for the alpha 2A-ligand binding site in human platelet and prejunctional potency in rat vas deferens (r = 0.90, n = 7, P less than 0.001), and submandibular gland (r = 0.84, n = 7, P less than 0.05). However, there was a better correlation between affinity for the alpha 2-ligand binding site of rat submandibular gland and prejunctional potency in rat vas deferens (r = 0.95, n = 7, P less than 0.001), and submandibular gland (r = 0.97, n = 7, P less than 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Smith K,Docherty JRdoi
10.1016/0014-2999(92)90297-hkeywords:
subject
Has Abstractpub_date
1992-08-25 00:00:00pages
203-10issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(92)90297-Hjournal_volume
219pub_type
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