Neuroleptic-like activity of peptides related to [DES-TYR1] γ-endorphin: Structure activity studies
Life SciencesPublished 1 May 1980Open access
D. de Wied, Jan M. van Ree, H. M. Greven
Citations99
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Abstract
The potency of various fragments of γ-endorphin (β-LPH61–77) was compared on their ability to facilitate extinction of pole-jumping avoidance behavior and their effects in two “grip tests” used as measures of neuroleptic-like activity. It appeared that β-LPH66–77 is the shortest sequence which shows potencies in the three tests comparable to that of DTγE (β-LPH62–77). The activity of β-LPH67–77 was less. It is proposed that β-LPH66–77 rather than DTγE represents an endogenous neuroleptic-like neuropeptide which may play a key role in psychopathology.
Keywords
MedicineNeuroscienceBiochemistry, Genetics and Molecular Biology
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298 Citations1978D. de Wied, Gábor L. Kovaćs +3 more
The results are interpreted to indicate that DTγE or a closely related peptide is an endogenous neuroleptic and may be that a reduced availability as a result of an inborn error in the generation ofDTγE is an etiological factor in psychopathological states for which Neuroleptic drugs are beneficial.
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58 Citations1979Michel Le Moal, George F. Koob +1 more
Alpha and gamma endorphin both inhibited the extinction of a runway task for water reward in water-deprived rats after subcutaneous injections of microgram dosages, suggesting that the effects of these peptides on motivated behavior may be situation-dependent.
European Journal of PharmacologyInhibition of in vivo 3H-spiperone binding by the proposed antipsychotic des-try1-γ-endorphin
46 Citations1979Norman W. Pedigo, Timothy Schallert +5 more
The proposed antipsychotic neuropeptide des-tyrosine1-gamma-endorphin (DT gamma E, beta LPH62,77) inhibits in vivo 3H-spiperone binding in the hypothalamus, corpus striatum and mesolimbic areas of rat brain, suggesting DT gamma E might act indirectly, having a selective neuroleptic-like action at 3h-spipersone binding sites.
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The inability of DTγE to inhibit specific 3 H-spiroperidol binding reported here suggests thatDTγE is not acting at the neuroleptic receptor labeled by 3 H -spiro peridol in these regions of rat brain.
