Agnostic about in Vivo Inverse Agonism of Agouti-Related Peptide

نویسندگان

چکیده

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

In vivo evidence for inverse agonism of Agouti-related peptide in the central nervous system of proopiomelanocortin-deficient mice.

OBJECTIVE Melanocyte-stimulating hormone (MSH) peptides processed from proopiomelanocortin (POMC) regulate energy homeostasis by activating neuronal melanocortin receptor (MC-R) signaling. Agouti-related peptide (AgRP) is a naturally occurring MC-R antagonist but also displays inverse agonism at constitutively active melanocortin-4 receptor (MC4-R) expressed on transfected cells. We investigate...

متن کامل

Effects of betahistine at histamine H3 receptors: mixed inverse agonism/agonism in vitro and partial inverse agonism in vivo.

We previously suggested that therapeutic effects of betahistine in vestibular disorders result from its antagonist properties at histamine H(3) receptors (H(3)Rs). However, H(3)Rs exhibit constitutive activity, and most H(3)R antagonists act as inverse agonists. Here, we have investigated the effects of betahistine at recombinant H(3)R isoforms. On inhibition of cAMP formation and [(3)H]arachid...

متن کامل

PHOSPHODIESTERASE INHIBITOR-DEPENDENT INVERSE AGONISM OF AGOUTI-RELATED PROTEIN (AGRP) ON MELANOCORTIN 4 RECEPTOR IN SEA BASS (Dicentrarchus labrax)

The melanocortin 4 receptor (MC4R) is a G-protein coupled receptor mainly expressed in the central nervous system of vertebrates. Activation of the MC4R leads to a decrease in food intake, while inactivating mutations are a genetic cause of obesity. The binding of agoutirelated protein (AGRP) reduces agonist-stimulated cAMP production (competitive antagonist) but also the basal activity of the ...

متن کامل

Phosphodiesterase inhibitor-dependent inverse agonism of agouti-related protein on melanocortin 4 receptor in sea bass (Dicentrarchus labrax).

The melanocortin 4 receptor (MC4R) is a G protein-coupled receptor mainly expressed in the central nervous system of vertebrates. Activation of the MC4R leads to a decrease in food intake, whereas inactivating mutations are a genetic cause of obesity. The binding of agouti-related protein (AGRP) reduces not only agonist-stimulated cAMP production (competitive antagonist) but also the basal acti...

متن کامل

Circulating Levels of Agouti-Related Peptide in Endometrial Cancer Survivors

Background Recently, it has been reported that central administration of agouti-related peptide (AgRP) might have protective effect against cachexia development in tumor-bearing mice. In this study, we determined whether the disease-free endometrial cancer survivors present with different plasma AgRP levels than controls and whether there was an association with the duration of the disease-free...

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

ژورنال

عنوان ژورنال: Endocrinology

سال: 2011

ISSN: 0013-7227,1945-7170

DOI: 10.1210/en.2011-0232