Dissociation of the cardiovascular and prolactin-releasing activities of norvaline2-TRH

Labroo, Virender M.; Cohen, Louis A.; Lozovsky, David; Sirén, Anna‐Leena; Feuerstein, Giora

doi:10.1016/0143-4179(87)90086-2

Cited by 8 publications

(2 citation statements)

References 21 publications

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“…TRH has multiple biological effects at various anatomical sites which may be mediated via different TRH receptor subtypes (22)(23)(24)(25). Previously, we have observed that backbone thionation of enkephalins yielded receptor-selective analogs (12,15).…”

Section: Resultsmentioning

confidence: 99%

Biological activities of thionated thyrotropin-releasing hormone analogs

Łankiewicz

Bowers

Reynolds

et al. 1992

Biochemical and Biophysical Research Communications

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SUMMARY:Analogs of thyrotropin-releasing hormone (Glp-His-Pro--NH2, TRH) have been prepared which contain thioamide moieties in the pyroglutamic acid ring, the carboxyamide proline terminus, andin both positions (dithio). These compounds have been tested für TSH-releasing activities (in vitro and in viuo), and for binding to TRH receptors in rat pituitary and cortex. The monothionated analoge showed no significant differences in TSH-releasing potency from TRH either in vitro or in vivo. However, with two thioamide replacements the potency decreases about 50%. Significantly, in terms of receptor selectivity, thionation has resulted in differentiation between brain receptors (p~tuitary and cortex). The Pro'V[CSNH2) and dithio analogs were more selective (higher affinity to pituitary receptors) than the parent hormone, while the analog containing a thioamide replacement in the pyroglutamyl ring had lower affinity and was not selective. These results suggest that the subtle exchange of sulphur for oxygen can have an important impact on both receptor selectivity and affinity within 8 biologically active peptide. 0 1992 Academic Press, Inc.

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Section: Resultsmentioning

confidence: 99%

Biological activities of thionated thyrotropin-releasing hormone analogs

Łankiewicz

Bowers

Reynolds

et al. 1992

Biochemical and Biophysical Research Communications

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“…Different substitutions at the two and four positions of the imidazole ring have produced compounds with more selective autonomie or endocrine activity, perhaps suggesting actions at separate populations of TRH isoreceptors (Feuerstein et al, 1984a;Siren et al, 1986;Labroo et al, 1987).…”

Section: Introductionmentioning

confidence: 97%

Imidazole-Substituted Analogues of TRH Limit Behavioral Deficits After Experimental Brain Trauma

Faden

Labroo²,

Cohen³

1993

Journal of Neurotrauma

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Treatment with thyrotropin releasing hormone (TRH) or TRH analogues improves outcome after experimental brain or spinal cord trauma. TRH analogues with modifications at the N-terminal position of the tripeptide are effective, whereas analogues with modifications of the C-terminal residue are not. Imidazole-substituted TRH analogues, which modify the middle amino acid (histidine) of the tripeptide, have more recently been developed but have not been evaluated in models of central nervous system (CNS) trauma. In the present studies two imidazole-substituted analogues--4(5)-NO2(Im)TRH and 2,4 diiodo(Im)TRH--are shown to improve behavioral recovery following fluid percussion-induced traumatic brain injury (TBI) in rats. Because 4(5)-NO2(Im)TRH has little endocrine activity and 2,4 diiodo(Im)TRH has minimal cardiovascular effects, these experiments support the hypothesis that the neuroprotective actions of TRH analogues are independent of their endocrine or autonomic actions.

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Biochemistry of halogenated organic compounds

Kirk¹

2009

Patai's Chemistry of Functional Groups

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Introduction Biohalogenation Biochemistry of the Thyroid Hormones Biochemistry of Selected Halogenated Organic Compounds Biochemistry of Polyhalogenated Organic Molecules Metabolism of Halogenated Organic Compounds—Biodehalogenation

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Dissociation of the cardiovascular and prolactin-releasing activities of norvaline2-TRH

Cited by 8 publications

References 21 publications

Biological activities of thionated thyrotropin-releasing hormone analogs

Biological activities of thionated thyrotropin-releasing hormone analogs

Imidazole-Substituted Analogues of TRH Limit Behavioral Deficits After Experimental Brain Trauma

Biochemistry of halogenated organic compounds

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