Abstract
The hypophysial homomeric peptide beta-lipotropin (beta-LPH-[1-91]) has no morphinomomimetic activity in a bioassay (myenteric plexus-longitudinal muscle of the guinea pig's ileum) or binding assays with stereospecific opiate-receptors of rat brain synaptosome preparations. Incubating beta-LPH-[1-91] at neutral pH with the supernatant aqueous extracts of rat brain generates (fragments of beta-LPH with) morphinomimetic activity in the same assay systems. These results are related to the recently recognized structural relationships between beta-LPH, the newly isolated peptides met-enkephalin (beta-LPH-[61-65]) and alpha-endorphin (beta-LPH-[61-76]) and also to the biologically active fragments of analogs: beta-LPH-[61-64], beta-LPH-[61-65[-NH2, (Met(O)65)-BETA-LPH-[61-65], beta-LPH-[61-69], and beta-LPH-[61-69]. Enzymatic biogenesis of these morphinomimetic peptides would preclude localizing them as such in cellular or subcellular elements with currently available methodology.
MeSH Terms
Amino Acid Sequence
Binding, Competitive
Brain/metabolism
Etorphine/metabolism
Ileum/drug effects
Morphine Derivatives/pharmacology
Naloxone/pharmacology
Nerve Tissue Proteins/biosynthesis,metabolism
Oligopeptides/biosynthesis,metabolism
Protein Precursors/metabolism
Receptors, Drug
Structure-Activity Relationship
beta-Lipotropin/metabolism
Chemicals
Morphine Derivatives
Nerve Tissue Proteins
Oligopeptides
Protein Precursors
Receptors, Drug
Naloxone
Etorphine
beta-Lipotropin
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Lazarus L H
Ling N
Guillemin R
References (21)
21 references, click to expand
-
THE RENIN-ANGIOTENSIN SYSTEM.
Pharmacol Rev. 1965 Jun;17:143-82
PMID: 14298579
-
LIPOTROPIN, A NEW ACTIVE PEPTIDE FROM PITUITARY GLANDS.
Nature. 1964 Feb 29;201:924
PMID: 14132790
-
On a possible role of beta-melanocyte stimulating hormone (beta-MSH) in the central nervous system of the Mammalia: enzymatic inactivation in vitro of beta-MSH by brain tissue.
Endocrinology. 1961 Jul;69:176-81
PMID: 13763329
-
The origin of acetylcholine released from guinea-pig intestine and longitudinal muscle strips.
J Physiol. 1968 Jan;194(1):13-33
PMID: 4295753
-
Narcotic receptor sites in morphine-dependent rats.
Nature. 1974 Mar 1;248(5443):61-3
PMID: 4131940
-
Biological proprtie of ovine beta-lipotropic hormone.
Endocrinology. 1968 May;82(5):898-904
PMID: 4171733
-
Renin activity in dog brain: enzymological similarity to cathepsin D.
Endocrinology. 1976 Jul;99(1):93-100
PMID: 181241
-
Adrenocorticotrophic and melanocyte-stimulating peptides in the human pituitary.
Biochem J. 1974 Jun;139(3):593-602
PMID: 4368382
-
Angiotensin-forming enzyme in human brain.
Neuropharmacology. 1975 Jan;14(1):75-80
PMID: 239362
-
Angiotensin-converting enzyme in human brain.
J Neurochem. 1975 Jul;25(1):83-5
PMID: 166145
-
Immunohistochemical and histochemical studies of pituitary beta-lipotrophs.
Anat Rec. 1973 Mar;175(3):529-37
PMID: 4349315
-
Angiotensin-forming enzyme in brain tissue.
Science. 1971 Jul 2;173(3991):64-5
PMID: 4325865
-
Commentary: behaviourally active ACTH analogues.
Biochem Pharmacol. 1975 Aug 15;24(16):1463-8
PMID: 172082
-
Synthesis of a pentekontapeptide with high lipolytic activity corresponding to the carboxyl-terminal fifty amino acids of ovine beta-lipotropin.
Proc Natl Acad Sci U S A. 1974 Dec;71(12):4945-9
PMID: 4531028
-
[Endorphins, hypothalamic and neurohypophysial peptides with morphinomimetic activity: isolation and molecular structure of alpha-endorphin].
C R Acad Sci Hebd Seances Acad Sci D. 1976 Feb 23;282(8):783-5
PMID: 817843
-
Isolation and structure of an untriakontapeptide with opiate activity from camel pituitary glands.
Proc Natl Acad Sci U S A. 1976 Apr;73(4):1145-8
PMID: 1063395
-
Opioid activity of a peptide, beta-lipotropin-(61-91), derived from beta-lipotropin.
Proc Natl Acad Sci U S A. 1976 Jun;73(6):1821-3
PMID: 1064855
-
Identification of two related pentapeptides from the brain with potent opiate agonist activity.
Nature. 1975 Dec 18;258(5536):577-80
PMID: 1207728
-
A peptide-like substance from pituitary that acts like morphine. 2. Purification and properties.
Life Sci. 1975 Jun 15;16(12):1777-82
PMID: 1152601
-
Inactivation of somatostatin (GH-RIH) and its an analogs by crude and partially purified rat brain extracts.
FEBS Lett. 1975 Jul 15;55(1):220-4
PMID: 1140419
-
The separation of synaptic vesicles from nerve-ending particles ('synaptosomes').
Biochem J. 1964 Feb;90(2):293-303
PMID: 5834239