Target intelligence / Profile preview

Amylin receptor 1 (AMY1R) (AMY1R)

Target
AMY1R
Molecular classification
G protein-coupled receptor, Class B GPCR, Heteromeric receptor complex
01

Overview

The Rat Amylin receptor 1 (AMY1R) is a functional heterodimeric G protein-coupled receptor formed by the association of the Calcitonin receptor (CTR) and the Receptor Activity-Modifying Protein 1 (RAMP1) [1][2]. In rats, this receptor complex is primarily expressed in the hindbrain, specifically the area postrema, where it mediates the anorectic effects of amylin, a peptide hormone co-secreted with insulin from pancreatic beta cells [3]. Activation of AMY1R leads to a reduction in food intake, slowing of gastric emptying, and suppression of postprandial glucagon secretion, making it a critical regulator of energy balance and glucose metabolism [2][4]. Due to its role in appetite control, AMY1R is a significant therapeutic target for the treatment of obesity and type 2 diabetes [5]. Synthetic amylin analogues, such as pramlintide and the long-acting cagrilintide, utilize this pathway to improve glycemic control and induce weight loss [5]. Understanding the specific pharmacology of the rat variant is essential for preclinical development of metabolic disease therapies [3].

Other names
AMY1CTR/RAMP1 complexCalcitonin receptor/Receptor activity-modifying protein 1 complexRat AMY1 receptor
02

Mechanism of action

Agonism of the AMY1R complex activates Gs-mediated signaling, increasing intracellular cAMP levels in the area postrema of the hindbrain, which induces satiety and slows gastric emptying.

03

Biological functions

Satiety signalingRegulation of gastric emptyingInhibition of glucagon secretionGlucose homeostasisBone metabolism regulation
04

Disease associations

ObesityType 2 diabetes mellitusHyperglycemia
05

Safety considerations

NauseaVomitingRisk of hypoglycemia when used with insulinInjection site reactions
06

Interacting drugs

Pramlintide

4 more in the full profile.

07

Biomarkers

Postprandial glucose levelsGastric emptying rateBody weight changeHbA1c

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