Analgesic activity of the naturally occurring heptapeptide [Met]enkephalin-Arg6-Phe7.

نویسندگان

  • C E Inturrisi
  • J G Umans
  • D Wolff
  • A S Stern
  • R V Lewis
  • S Stein
  • S Udenfriend
چکیده

[Met]Enkephalin-Arg6-Phe7 is an opiate-like peptide normally found in the the adrenal gland and brain that has analgesic (antinociceptive) activity when administered directly into the cerebral ventricles of mice. On a molar basis, [Met]-enkephalin-Arg6-Phe7, with a median effective dose (ED50) of 38.5 nmol/mouse, is 8 times more potent than [Met]enkephalin. As with [Met]enkephalin, analgesic activity is blocked by naloxone and intravenous administration does not produce characteristic opiate effects in tests for analgesic, antidiuretic, or antidiarrheal activity. These findings suggest that [Met]enkephalin-Arg6-Phe7 may be at least as important as the enkephalins in the postulated enkephalin system mediating pain and analgesia.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Effect of endogenous opioid peptides on acetylcholine release from the cat superior cervical ganglion: selective effect of a heptapeptide.

The present experiments show the presence of both metenkephalin-like and met-enkephalin-Arg6-Phe7-like immunoreactivity in the superior cervical ganglion of the cat; this was determined by radioimmunoassay after high-pressure liquid chromatography separation of tissue extracts. There was measurable efflux of both peptides, as determined by radioimmunoassay of ganglionic perfusates; this measure...

متن کامل

Immunocytochemical demonstration of the co-storage of noradrenaline with Met-enkephalin-Arg6-Phe7 and Met-enkephalin-Arg6-Gly7-Leu8 in the carotid body chief cells of the dog.

Cellular and ultrastructural localization of catecholamines in the dog carotid body was investigated by peroxidase-antiperoxidase method for light microscopy and by protein A-colloidal gold technique for electron microscopy, and compared with that of preproenkephalin A-related opioid peptides, i.e., Met-enkephalin-Arg6-Phe7 (Met-Enk-Arg-Phe) and Met-enkephalin-Arg6-Gly7-Leu8 (Met-Enk-Arg-Gly-Le...

متن کامل

Processing of enkephalin-containing peptides in isolated bovine adrenal chromaffin granules.

Intact chromaffin granules isolated from bovine adrenal medulla were incubated at 37 degrees C for up to 22 hr. Processing of enkephalin-containing (EC) peptides in the granules was followed by the change in their size distribution as shown by chromatography on Sephadex G-75 columns. A gradual shift toward lower molecular weight EC peptides was observed during the incubation, indicating process...

متن کامل

Intact proenkephalin is the major enkephalin-containing peptide produced in rat adrenal glands after denervation.

We have shown previously that enkephalin-containing peptides of high molecular weight increase 10- to 15-fold 3 days after adrenal denervation and have suggested that much of this material may represent newly synthesized proenkephalin. In this paper we report that most of the material appearing after denervation is indeed intact proenkephalin. The putative proenkephalin was partially purified b...

متن کامل

Alteration in endogenous opioid systems due to chronic inflammatory pain conditions.

The influence of chronic arthritic pain on two endogenous opioid peptides, dynorphin B and [Met5]enkephalin-Arg6-Phe7, and multiple opioid receptors in discrete brain, lumbar spinal cord and pituitary pools was investigated. Using radioimmunoassay and receptor binding assay, we examined the changes in regional opioid peptide levels and opioid receptor activity due to chronic inflammation in adj...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Proceedings of the National Academy of Sciences of the United States of America

دوره 77 9  شماره 

صفحات  -

تاریخ انتشار 1980