Tachykinin antagonist I: Specific, competitive and tissue-selective neurokinin B antagonists on contractile activity in smooth muscles.

نویسندگان

  • T Hashimoto
  • Y Uchida
  • S Naminohira
  • T Sakai
چکیده

Two neurokinin B (NKB) analogs, [Gly6]-NKB [3-10] and [Arg3, D-Ala6]-NKB [3-10], were tested for agonistic activity as well as for their ability to antagonize the myotropic actions of NKB, neurokinin A, substance P, physalaemin and eledoisin in isolated guinea-pig ileum, guinea-pig urinary bladder, rat duodenum, rat vas deferens and rat portal vein. [Gly6]-NKB [3-10] in the guinea-pig ileum and rat portal vein and [Arg3, D-Ala6]-NKB [3-10] in the guinea-pig ileum were found to be the first specific and competitive antagonists against NKB.

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

Expression and coupling of neurokinin receptor subtypes to inositol phosphate and calcium signaling pathways in human airway smooth muscle cells.

Neuropeptide tachykinins (substance P, neurokinin A, and neurokinin B) are present in peripheral terminals of sensory nerve fibers within the respiratory tract and cause airway contractile responses and hyperresponsiveness in humans and most mammalian species. Three subtypes of neurokinin receptors (NK1R, NK2R, and NK3R) classically couple to Gq protein-mediated inositol 1,4,5-trisphosphate (IP...

متن کامل

beta(2)-adrenoceptor agonist-induced upregulation of tachykinin NK(2) receptor expression and function in airway smooth muscle.

Neurokinin A (NKA) induces bronchoconstriction mediated by tachykinin NK(2) receptors in animals and humans, and may be increased in asthma. Because beta(2)-adrenoceptor agonists are the most widely used bronchodilators in asthma, we investigated the effects of the beta(2)-adrenoceptor agonist fenoterol on NK(2) receptor messenger RNA (mRNA) and receptor density as well as the functional respon...

متن کامل

Structure-Activity Study of Guinea Pig Trachea Tachykinin NK-2 Receptor: Effect of Substitution at the Seventh Position from C-Terminus of Neurokinin A

Substance P (SP: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-GlyLeu-Met-NH2), neurokinin A (NKA: His-Lys-Thr-Asp-ThrPhe-Val-Gly-Leu-Met-NH2) and neurokinin B (NKB: AspMet-His-Asp-Phe-Phe-Val-Gly-Leu-Met-NH2) are mammalian tachykinin peptides that have similar biological actions, such as smooth muscle contraction, salivation, vasodilatation and neuronal excitation. These mammalian tachykinin peptides are ch...

متن کامل

Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of tachykinin NK-1 and NK-2 receptors agonists and antagonists.

OBJECTIVES Present experiments were undertaken to study the influence of peptide NK-1 and NK-2 receptor agonists and antagonists as well as substance P and neurokinin A (the natural ligands for these tachykinin receptors) on vasopressin (AVP) secretion from the rat hypothalamo-neurohypophysial (HN) system in vitro. RESULTS The results showed that both substance P and highly selective tachykin...

متن کامل

Autocrine regulation of human sperm motility by tachykinins

BACKGROUND We examined the presence and function of tachykinins and the tachykinin-degrading enzymes neprilysin (NEP) and neprilysin-2 (NEP2) in human spermatozoa. METHODS Freshly ejaculated semen was collected from forty-eight normozoospermic human donors. We analyzed the expression of substance P, neurokinin A, neurokinin B, hemokinin-1, NEP and NEP2 in sperm cells by reverse-transcriptase ...

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:
  • Japanese journal of pharmacology

دوره 45 4  شماره 

صفحات  -

تاریخ انتشار 1987