1978
DOI: 10.1111/j.1476-5381.1978.tb08653.x
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Rat Vas Deferens: A Specific Bioassay for Endogenous Opioid Peptides

Abstract: The electrically‐evoked contractions of the rat vas deferens were selectively inhibited by β‐endorphin, the preparation being much less sensitive to enkephalins and narcotic analgesic drugs. However, introduction of D‐Ala in position 2 of [Leu]‐enkephalin enhanced the activity of the opioid peptide to the order of that of β‐endorphin. It is concluded that the rat vas deferens preparation constitutes a specific bioassay for endogenous opioid peptides and related compounds.

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Cited by 111 publications
(31 citation statements)
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“…Another interesting finding observed in the present study is the fact that the IC50 ratio in the presence to in the absence of sodium of dynorphin- (1-1 3), which had been shown to be a strong kappa agonist (13), was less than those of mixed agonist-antagonists and significantly low when it was compared to those of other opioid agonists. This character of dynorphin- (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13) may relate to its peculiar antagonistic action (22). Inter estingly, the IC50 ratio in the presence to in the absence of sodium of ketocyclazocine, which had been reported to behave as an effective antagonist as well as a potent agonist in the guinea-pig ileum (23), was also low.…”
Section: Discussionmentioning
confidence: 99%
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“…Another interesting finding observed in the present study is the fact that the IC50 ratio in the presence to in the absence of sodium of dynorphin- (1-1 3), which had been shown to be a strong kappa agonist (13), was less than those of mixed agonist-antagonists and significantly low when it was compared to those of other opioid agonists. This character of dynorphin- (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13) may relate to its peculiar antagonistic action (22). Inter estingly, the IC50 ratio in the presence to in the absence of sodium of ketocyclazocine, which had been reported to behave as an effective antagonist as well as a potent agonist in the guinea-pig ileum (23), was also low.…”
Section: Discussionmentioning
confidence: 99%
“…Additionally, the reduction of the potency of dynorphin-(1 13) was quite small in the presence of sodium alone, while it was large in the presence of both Gpp(NH)p and sodium (Table 4). Interestingly, the chemical structure of either U-50,488, dynorphin- (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13) or tifluadom is quite different from that of traditional benzomorphan kappa agonists such as ketocyclazocine and ethylketocyclazocine (12)(13)(14).…”
Section: Abstract-effects Of 5'-guanylylimidodiphosphate (Gpp(nh)p) Amentioning
confidence: 99%
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“…A new type of opiate receptor, e-receptor, has been postulated to be present in this tissue (3). Extensive studies mainly focused on the agonist potency have provided many data concerning the characteristics of e-receptor (1)(2)(3)(4)(5). However, the question of why mor phine and many other opiate agonists are ineffective in the rat vas deferens remains unknown.…”
mentioning
confidence: 99%
“…The rat vas deferens is highly sensitive to 8-endorphin, but practically insensitive to morphine (1,2). On account of these unique properties, this tissue has been given much attention in recent years.…”
mentioning
confidence: 99%