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d-Lys-GHRP-6 does not modify the endocrine response to acylated ghrelin or hexarelin in humans.
Neuropeptides. 2007 Feb; 41(1):45-9.N

Abstract

Acylated ghrelin exerts numerous endocrine and non-endocrine activities via the GH Secretagogue receptor type 1a (GHS-R1a). D-Lys-GHRP-6 has been widely studied in vitro and in vivo in animal studies as GHS-R1a antagonist; its action in humans has, however, never been tested so far. Aim of our study was to verify the antagonistic action of D-Lys-GHRP-6 on the endocrine responses to acylated ghrelin and hexarelin, a peptidyl synthetic GHS, in humans. The effects of different doses of D-Lys-GHRP-6 (2.0microg/kg iv as bolus or 2.0microg/kg/h iv as infusion) on both spontaneous and acylated ghrelin- or hexarelin (1.0microg/kg iv as bolus) -stimulated GH, PRL, ACTH and cortisol levels were studied in six normal volunteers (age [mean+/-SEM]: 25.4+/-1.2yr; BMI: 22.3+/-1.0kg/m(2)). The effects of D-Lys-GHRP-6 (2.0microg/kg iv as bolus+4.0microg/kg/h iv) on the GH response to 0.25microg/kg iv as bolus acylated ghrelin was also studied. During saline, spontaneous ACTH and cortisol decrease was observed while non changes occurred in GH and PRL levels. Acylated ghrelin and hexarelin stimulated (p<0.05) GH, PRL, ACTH and cortisol secretions. D-Lys-GHRP-6 administered either as bolus or a continuous infusion did not modify both spontaneous and acylated ghrelin- or hexarelin-stimulated GH, PRL, ACTH and cortisol secretion. D-Lys-GHRP-6 did not modify even the GH response to 0.25microg/kg iv acylated ghrelin. In conclusion, D-Lys-GHRP-6 does not affect the neuroendocrine response to both ghrelin and hexarelin. These findings question D-Lys-GHRP-6 as an effective GHS-R1a antagonist for human studies.

Authors+Show Affiliations

Division of Endocrinology and Metabolism, Department of Internal Medicine, University of Turin, Turin, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17112585

Citation

Benso, A, et al. "D-Lys-GHRP-6 Does Not Modify the Endocrine Response to Acylated Ghrelin or Hexarelin in Humans." Neuropeptides, vol. 41, no. 1, 2007, pp. 45-9.
Benso A, Prodam F, Lucatello B, et al. D-Lys-GHRP-6 does not modify the endocrine response to acylated ghrelin or hexarelin in humans. Neuropeptides. 2007;41(1):45-9.
Benso, A., Prodam, F., Lucatello, B., Gramaglia, E., Riganti, F., Schneider, H., van der Lely, A. J., Muccioli, G., Ghigo, E., & Broglio, F. (2007). D-Lys-GHRP-6 does not modify the endocrine response to acylated ghrelin or hexarelin in humans. Neuropeptides, 41(1), 45-9.
Benso A, et al. D-Lys-GHRP-6 Does Not Modify the Endocrine Response to Acylated Ghrelin or Hexarelin in Humans. Neuropeptides. 2007;41(1):45-9. PubMed PMID: 17112585.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - d-Lys-GHRP-6 does not modify the endocrine response to acylated ghrelin or hexarelin in humans. AU - Benso,A, AU - Prodam,F, AU - Lucatello,B, AU - Gramaglia,E, AU - Riganti,F, AU - Schneider,H, AU - van der Lely,A J, AU - Muccioli,G, AU - Ghigo,E, AU - Broglio,F, Y1 - 2006/11/16/ PY - 2006/08/17/received PY - 2006/10/02/revised PY - 2006/10/03/accepted PY - 2006/11/23/pubmed PY - 2007/8/7/medline PY - 2006/11/23/entrez SP - 45 EP - 9 JF - Neuropeptides JO - Neuropeptides VL - 41 IS - 1 N2 - Acylated ghrelin exerts numerous endocrine and non-endocrine activities via the GH Secretagogue receptor type 1a (GHS-R1a). D-Lys-GHRP-6 has been widely studied in vitro and in vivo in animal studies as GHS-R1a antagonist; its action in humans has, however, never been tested so far. Aim of our study was to verify the antagonistic action of D-Lys-GHRP-6 on the endocrine responses to acylated ghrelin and hexarelin, a peptidyl synthetic GHS, in humans. The effects of different doses of D-Lys-GHRP-6 (2.0microg/kg iv as bolus or 2.0microg/kg/h iv as infusion) on both spontaneous and acylated ghrelin- or hexarelin (1.0microg/kg iv as bolus) -stimulated GH, PRL, ACTH and cortisol levels were studied in six normal volunteers (age [mean+/-SEM]: 25.4+/-1.2yr; BMI: 22.3+/-1.0kg/m(2)). The effects of D-Lys-GHRP-6 (2.0microg/kg iv as bolus+4.0microg/kg/h iv) on the GH response to 0.25microg/kg iv as bolus acylated ghrelin was also studied. During saline, spontaneous ACTH and cortisol decrease was observed while non changes occurred in GH and PRL levels. Acylated ghrelin and hexarelin stimulated (p<0.05) GH, PRL, ACTH and cortisol secretions. D-Lys-GHRP-6 administered either as bolus or a continuous infusion did not modify both spontaneous and acylated ghrelin- or hexarelin-stimulated GH, PRL, ACTH and cortisol secretion. D-Lys-GHRP-6 did not modify even the GH response to 0.25microg/kg iv acylated ghrelin. In conclusion, D-Lys-GHRP-6 does not affect the neuroendocrine response to both ghrelin and hexarelin. These findings question D-Lys-GHRP-6 as an effective GHS-R1a antagonist for human studies. SN - 0143-4179 UR - https://www.unboundmedicine.com/medline/citation/17112585/d_Lys_GHRP_6_does_not_modify_the_endocrine_response_to_acylated_ghrelin_or_hexarelin_in_humans_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0143-4179(06)00116-8 DB - PRIME DP - Unbound Medicine ER -