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L-368,899
L-368,899 is a drug used in scientific research which acts as a selective antagonist of the oxytocin receptor, with good selectivity over the related vasopressin receptors. Unlike related drugs such as the peripherally selective L-371,257, the oral bioavailabity is high and the brain penetration of L-368,899 is rapid, with selective accumulation in areas of the limbic system. This makes it a useful tool for investigating the centrally mediated roles of oxytocin, such as in social behaviour and pair bonding, and studies in primates have shown L-368,899 to reduce a number of behaviours such as food sharing, sexual activity and caring for infants, demonstrating the importance of oxytocinergic signalling in mediating these important social behaviours. See also * Atosiban * Barusiban * Epelsiban * L-371,257 * Retosiban Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxytocin Receptor
The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. In humans, the oxytocin receptor is encoded by the ''OXTR'' gene which has been localized to human chromosome 3p25. Function and location The OXTR protein belongs to the G-protein coupled receptor family, specifically Gq, and acts as a receptor for oxytocin. Its activity is mediated by G proteins that activate several different second messenger systems. Oxytocin receptors are expressed by the myoepithelial cells of the mammary gland, and in both the myometrium and endometrium of the uterus at the end of pregnancy. The oxytocin-oxytocin receptor system plays an important role as an inducer of uterine contractions during parturition and of milk ejection. OXTR is also associated with the central nervous system. The gene is believed to play a major role in social, cognitive, and emotional behavior. A decrease in OXTR expression by methylation of th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
L-371,257
L-371,257 is a compound used in scientific research which acts as a selective antagonist of the oxytocin receptor with over 800x selectivity over the related vasopressin receptors. It was one of the first non-peptide oxytocin antagonists developed, and has good oral bioavailability, but poor penetration of the blood–brain barrier, which gives it good peripheral selectivity with few central side effects. Potential applications are likely to be in the treatment of premature labour. See also * Atosiban * Barusiban * Epelsiban * L-368,899 L-368,899 is a drug used in scientific research which acts as a selective antagonist of the oxytocin receptor, with good selectivity over the related vasopressin receptors. Unlike related drugs such as the peripherally selective L-371,257, the ora ... * Retosiban References {{Oxytocin and vasopressin receptor modulators Tocolytics Oxytocin receptor antagonists Peripherally selective drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Barusiban
Barusiban (INN) (code name FE-200440) is a non-peptide drug which is among the most potent and selective oxytocin receptor antagonists known. It was trialed by Ferring Pharmaceuticals as a treatment of preterm labor but failed to demonstrate effectiveness and was not pursued any further. See also * Atosiban * Epelsiban * L-368,899 * L-371,257 * Retosiban Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour. Retosiban has high affinity for the oxytocin receptor (Ki = 0.65 ... References {{Oxytocin and vasopressin receptor modulators Abandoned drugs Carboxamides Tryptamines Oxytocin receptor antagonists Tocolytics ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Epelsiban
Epelsiban ( INN, USAN, code name GSK-557,296-B) is an orally bioavailable drug which acts as a selective and potent oxytocin receptor antagonist ( Ki = 0.13 nM). It was initially developed by GlaxoSmithKline (GSK) for the treatment of premature ejaculation in men and then as an agent to enhance embryo or blastocyst implantation in women undergoing embryo or blastocyst transfer associated with ''in vitro'' fertilization ( IVF)., and was also investigated for use in the treatment of adenomyosis. Discovery and Design Screening the GSK compound collection and various libraries identified 2,5-diketopiperazines (2,5-DKPs) exemplified by 1 as novel and selective antagonists at the human oxytocin receptor (OTR). The lead, 1, showed potency of Ki = 300nM as a mixture of isomers in the amide side-chain. Initial structure–activity relationship (SAR) studies led to the semi-rigid and chirally pure 2,5-DKP 2 (Ki = 4nM), with ''cis'' disposed substituents at C-3 and C-6 and the ''R'' si ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Retosiban
Retosiban also known as GSK-221,149-A is an oral drug which acts as an oxytocin receptor antagonist. It is being developed by GlaxoSmithKline for the treatment of preterm labour. Retosiban has high affinity for the oxytocin receptor (Ki = 0.65 nM) and has greater than 1400-fold selectivity over the related vasopressin receptors Mechanism of action Retosiban is a competitive oxytocin receptor antagonist which blocks the oxytocin-mediated contraction of the uterine smooth muscle in the female uterus that occurs during the initiation of preterm labour. This has been used to prevent preterm labour and premature birth. Pharmacology Retosiban has been shown to be an effective tocolytic. By intravenous and oral administration it produces a dose-dependent decrease in oxytocin-induced uterine contractions in non-pregnant female rats. In late-term pregnant rats it significantly reduces spontaneous uterine contractions in a dose-dependent manner by intravenous administration. In humans ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antagonist (pharmacology)
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Vasopressin Receptor
The actions of vasopressin are mediated by stimulation of tissue-specific G protein-coupled receptors (GPCRs) called vasopressin receptors that are classified into the V1 (V1A), V2, and V3 (V1B) receptor subtypes. These three subtypes differ in localization, function and signal transduction mechanisms. Subtypes There are three subtypes of vasopressin receptor: V1A (V1), V1B (V3) and V2. V1 receptor V1 receptors (V1Rs) are found in high density on vascular smooth muscle and cause vasoconstriction by an increase in intracellular calcium via the phosphatidyl–inositol-bisphosphate cascade. Cardiac myocytes also possess V1R. Additionally V1R are located in brain, testis, superior cervical ganglion, liver, blood vessels, and renal medulla. V1R is present on platelets, which upon stimulation induces an increase in intracellular calcium, facilitating thrombosis. Studies have indicated that due to polymorphism of platelet V1R there is significant heterogeneity in the aggrega ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Limbic System
The limbic system, also known as the paleomammalian cortex, is a set of brain structures located on both sides of the thalamus, immediately beneath the medial temporal lobe of the cerebrum primarily in the forebrain.Schacter, Daniel L. 2012. ''Psychology''.sec. 3.20 It supports a variety of functions including emotion, behavior, long-term memory, and olfaction. Emotional life is largely housed in the limbic system, and it critically aids the formation of memories. With a primordial structure, the limbic system is involved in lower order emotional processing of input from sensory systems and consists of the amygdaloid nuclear complex (amygdala), mammillary bodies, stria medullaris, central gray and dorsal and ventral nuclei of Gudden. This processed information is often relayed to a collection of structures from the telencephalon, diencephalon, and mesencephalon, including the prefrontal cortex, cingulate gyrus, limbic thalamus, hippocampus including the parahippocampal gyrus an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pair Bond
In biology, a pair bond is the strong affinity that develops in some species between a mating pair, often leading to the production and rearing of offspring and potentially a lifelong bond. Pair-bonding is a term coined in the 1940s that is frequently used in sociobiology and evolutionary biology circles. The term often implies either a lifelong socially monogamous relationship or a stage of mating interaction in socially monogamous species. It is sometimes used in reference to human relationships. Varieties According to evolutionary psychologists David P. Barash and Judith Lipton, from their 2001 book ''The Myth of Monogamy'', there are several varieties of pair bonds: *''Short-term pair-bond:'' a transient mating or associations *''Long-term pair-bond:'' bonded for a significant portion of the life cycle of that pair *''Lifelong pair-bond:'' mated for life *''Social pair-bond:'' attachments for territorial or social reasons *''Clandestine pair-bond:'' quick extra-pair copulati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atosiban
Atosiban, sold under the brand name Tractocile among others, is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. It was developed by Ferring Pharmaceuticals in Sweden and first reported in the literature in 1985. Originally marketed by Ferring Pharmaceuticals, it is licensed in proprietary and generic forms for the delay of imminent preterm birth in pregnant adult women. The most commonly reported side effect is nausea. Medical uses Atosiban is used to delay birth in adult women who are 24 to 33 weeks pregnant, when they show signs that they may give birth pre-term (prematurely). These signs include regular contractions lasting at least 30 seconds at a rate of at least four every 30 minutes, and dilation of the cervix (the neck of the womb) of 1 to 3 cm and an effacement (a measure of the thinness of the cervix) of 50% or more. In addition, the baby must have a normal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxytocin Receptor Antagonists
Oxytocin (Oxt or OT) is a peptide hormone and neuropeptide normally produced in the hypothalamus and released by the posterior pituitary. It plays a role in social bonding, reproduction, childbirth, and the period after childbirth. Oxytocin is released into the bloodstream as a hormone in response to sexual activity and during labour. It is also available in pharmaceutical form. In either form, oxytocin stimulates uterine contractions to speed up the process of childbirth. In its natural form, it also plays a role in bonding with the baby and milk production. Production and secretion of oxytocin is controlled by a positive feedback mechanism, where its initial release stimulates production and release of further oxytocin. For example, when oxytocin is released during a contraction of the uterus at the start of childbirth, this stimulates production and release of more oxytocin and an increase in the intensity and frequency of contractions. This process compounds in intensity ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
