Last update 19 Sep 2024

CCKA

Last update 19 Sep 2024

Basic Info

Synonyms

胆囊收缩素A受体, CCK-A receptor, CCK-AR

+ [6]

Introduction

Receptor for cholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.

Drugs associated with CCKA

Sincalide

Target

CCKA x CCKB

Mechanism

CCKA agonists [+1]

Active Org.

Maia Pharmaceuticals, Inc. [+1]

Originator Org.

Bracco International BV

Active Indication

Gallbladder Diseases [+3]

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date21 Jul 1976

PNB-001

Target

CCKA x CCKB

Mechanism

CCKA antagonists [+1]

Active Org.

PNB Vesper Life Sciences Pvt. Ltd

Originator Org.

PNB Vesper Life Sciences Pvt. Ltd

Active Indication

COVID-19 [+2]

Inactive Indication-

Drug Highest PhasePhase 3

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Dexloxiglumide

Target

CCKA

Mechanism

CCKA antagonists

Active Org.

Rottapharm SpA [+1]

Originator Org.

Rottapharm SpA

Active Indication

Irritable Bowel Syndrome

Inactive Indication

Dyspepsia [+2]

Drug Highest PhasePhase 3

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with CCKA

CTRI/2022/10/046658 / RecruitingPhase 2

A Phase II, Multicenter, Randomized, Double-blind, Placebo controlled Clinical study toevaluate efficacy and safety of PNB-001 as an adjunct to Mesalamine compared toMesalamine alone in Subjects with Inflammatory bowel disease

Start Date28 Oct 2022

Sponsor / Collaborator

PNB Vesper Life Sciences Pvt. Ltd

[+1]

CTRI/2021/09/036411 / RecruitingPhase 3

A Phase III, Randomized, Open Label, Multicentric, Clinical Study to Evaluate the Efficacy and Safety of PNB-001 as an Adjunct to Standard of Care Compared to Standard of Care Alone in Treatment of Patients with Moderate COVID-19 Infection

Start Date27 Sep 2021

Sponsor / Collaborator

PNB Vesper Life Sciences Pvt. Ltd

CTRI/2020/10/028423 / CompletedPhase 2

A Randomized, Open label Clinical Study to Evaluate Efficacy and Safety of PNB-001 in Patients with moderate COVID-19 Infection.

Start Date28 Oct 2020

Sponsor / Collaborator

PNB Vesper Life Sciences Pvt. Ltd

[+1]

100 Clinical Results associated with CCKA

100 Translational Medicine associated with CCKA

0 Patents (Medical) associated with CCKA

1,071

Literatures (Medical) associated with CCKA

01 Sep 2024·Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology

Effects of fasting and environmental factors on appetite regulators in pond loach Misgurnus anguillicaudatus

Article

Author: Lindstrom, Annika ; Volkoff, Helene ; Kuhn, Jannik

The pond loach (Misgurnus anguillicaudatus) is an important aquaculture freshwater species, used as an ornamental fish, food source for humans and angling bait. Pond loaches are resistant to fasting and extreme environmental conditions, including temperature and low oxygen levels. Little is known about how these factors affect the feeding physiology and the endocrine regulation of feeding of loaches. In this study, we examined the effects of fasting, as well as increased temperature and decreased oxygen levels on food intake and transcript levels of appetite regulators. Fasted fish had lower blood glucose levels, and lower expression levels of intestine CCK and PYY, and brain CART1, but had higher levels of brain orexin and ghrelin than fed fish. Fish held at 30 °C had higher food intake, glucose levels, and mRNA levels of intestine CCK and PYY, and brain CART2, but lower brain orexin levels than fish at 20 °C. Fish held at low oxygen levels had a lower food intake, higher intestine CCKa and ghrelin, and brain orexin, CART2 and ghrelin mRNA expression levels than fish held at high O₂ levels. Our results suggest that fasting and high temperatures increase the expression of orexigenic and anorexigenic factors respectively, whereas the increase in expression of both orexigenic and anorexigenic factors in low O₂ environments might not be related to their role in feeding, but possibly to protection from tissue damage. The results of our study might shed new light on how pond loaches are able to cope with extreme environmental conditions such as low food availability, extreme temperatures and hypoxia.

01 Aug 2024·European Journal of Pharmaceutical Sciences

Discovery of novel glucagon-like peptide 1/cholecystokinin 1 receptor dual agonists

Article

Author: Binbin, Gong ; Qian, Long ; Ting, Wang ; Lidan, Sun ; Guoqiang, Hu ; Xiaoyi, Sun ; Chenxu, Zhou

The combined use of gastrointestinal hormones for treating metabolic diseases is gaining increasing attention. The potential of developing novel dual agonists targeting both cholecystokinin 1 (CCK-1) receptor and glucagon-like peptide 1 (GLP-1) receptor to improve the treatment of type 2 diabetes and obesity have not been fully explored. In this investigation, we reported a series of novel GLP-1/CCK-1 receptor co-agonists constructed by linking the C-terminus of a GLP-1 receptor agonist (bullfrog GLP-1) to the N-terminus of a CCK-1 receptor selective agonist NN9056. In comprehensive in vitro assays, these co-agonists exhibited complete agonistic potency on GLP-1 and CCK-1 receptor. Remarkably, 1f displayed superior hypoglycemic and insulinotropic effects when compared to NN9056 and semaglutide. Evaluation in Kunming and diet-induced obesity (DIO) mice unveiled significant acute and enduring hypoglycemic effects of 1f. Administration of 1f to DIO mice resulted in substantial weight loss, normalized lipid metabolism, and enhanced glucose regulation. These preclinical observations strongly advocate for the therapeutic potential CCK-1 and GLP-1 pathways could be harnessed in a single fusion peptide, yielding a promising combination therapy strategy for treating metabolic disorders.

01 May 2024·Reproduction in Domestic Animals

Cholecystokinin‐mediated effect of insulin pathway on the steroidogenic activity of follicular granulosa cells in Camelus bactrianus: In vitro study

Article

Author: Guo, Lusha ; Zhang, Yong

AbstractThe current study aimed to explore the molecular mechanism by which the cholecystokinin (CCK)‐mediated CCKAR and CCKBR, as well as the molecular mechanisms of CCK‐mediated insulin signalling pathway, regulate oestrogen in the granulosa cells. Also, the expression of CCK in ovaries, uterus, hypothalamus and pituitary gland was investigated in Camelus bactrianus. Ovaries, uterus, hypothalamus and pituitary gland were collected from six, three before ovulation (control) and three after ovulation, slaughtered Camelus bactrianus. Ovulation was induced by IM injection of seminal plasma before slaughtering in the ovulated group. The results showed that there were differences in the transcription and protein levels of CCK in various tissues before and after ovulation (p < .05, p < .01). After transfection with p‐IRES2‐EGFP‐CCK, the mRNA and protein levels of CCK, CCKAR, CCKBR and ER in follicular granulosa cells were significantly upregulated (p < .05, p < .01), and the content of E2 was significantly upregulated (p < .01); On the contrary, after transfection with si‐CCK, the mRNA and protein levels of CCK, CCKAR, CCKBR and ER in follicular granulosa cells were significantly downregulated (p < .05, p < .01), and the content of E2 was significantly downregulated (p < .01). Regulating CCK can affect the mRNA levels of INS, INSR, IGF and IGF‐R. In summary, regulating the expression level of CCK can activate insulin‐related signalling pathways by CCKR, thereby regulating the steroidogenic activity of granulosa cells.

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CCKA

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