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Vasopressin and Oxytocin Family Related Drug Discovery Products

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In mammals, including humans, the neuropeptides vasopressin (VP) and oxytocin (OT), are involved in the regulation of a variety of social activities, including social recognition, pair-bonding, and social cognition. With only two amino acids separating them, VP and OT are evolutionarily conserved. It is significant to note that VP and OT have been linked to the etiology of mental conditions such schizophrenia, autism, depression, and borderline personality disorder, conditions that exhibit sex biases in prevalence, symptom severity, and treatment outcomes. Therefore, understanding the variations between the sexes in these systems, as well as how OT and VP may affect sex-specific social behavior, may be helpful in developing sex-specific treatment plans for both men and women who have been diagnosed with psychiatric disorders that include social dysfunction.

Oxytocin and vasopressin. Fig.1. Oxytocin and vasopressin. (Bordt, 2019)

Creative Biolabs provides vasopressin and oxytocin family in vitro assays and related products to facilitate our customers' development of membrane protein drugs:

Overview of Vasopressin and Oxytocin Family

  • AVPR1A

Animal studies have shown that vasopressin has an anorectic effect. AVP functions as a neurotransmitter or neuromodulator in the brain, stimulating ventromedial glucose-responsive neurons in the hypothalamus and paraventricular nucleus neurons. AVP also seems to influence the impact of orexins and other neuropeptides on eating behavior. The link between AVPR1a and eating disorders may be a result of this receptor's function as a mediator of a variety of social behaviors in people.

The AVPR1A gene. Fig.2. The AVPR1A gene. (Ebstein, 2012)

  • AVPR1B

The anterior lobe corticotrophs of the pituitary gland are where AVPR1b is mostly found. As part of the neuroendocrine response to stress, AVP in hypophysial portal blood interacts with pituitary AVPR1b to produce adrenocorticotrophic hormone (ACTH). There is evidence that AVPR1b receptors are found in the hypothalamus, amygdala, and cerebellum, among other regions of the brain. The area-specific distribution of this receptor may be influenced by components in the AVPR1b promoter region. Numerous research have investigated the relationship between human stress, antidepressant therapy, childhood mood disorders, and ADHD and the AVPR1b receptor.

  • AVPR2

When activated by its agonist, arginine vasopressin (AVP), AVPR2, speeds up the reabsorption of water into the renal collecting tubules. In response to hypovolemia or high osmolality, the posterior pituitary secretes AVP, which binds to AVPR2 in the basolateral membrane of these main cells. Adenylyl cyclase is thought to be stimulated by the binding of AVP at transmembrane helix II–IV through the stimulatory G protein (Gs). This encourages the water channel AQP-2 to move into the luminal membrane via the cAMP/PKA pathway, allowing water to enter easily through the medullary osmotic gradien.

The AVPR2 receptor signaling cascade. Fig.3. The AVPR2 receptor signaling cascade. (Makita, 2020)

References

  1. Bordt, E.A.; et al. Mitochondria, oxytocin, and vasopressin: unfolding the inflammatory protein response. Neurotoxicity research. 2019, 36: 239-256.
  2. Ebstein, R.P.; et al. The contributions of oxytocin and vasopressin pathway genes to human behavior. Hormones and behavior. 2012, 61(3): 359-379.
  3. Makita, N.; et al. V2 vasopressin receptor mutations. Vitamins and Hormones. 2020, 113: 79-99.

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