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Non-ergoline dopamine receptor agonists have higher binding affinity to dopamine D 3-receptors than dopamine D 2-receptors. This binding affinity is related to D 2 and D 3 receptor homology, the homology between them has a high degree of sequence and is closest in their transmembrane domains, were they share around 75% of the amino acid. [37]
Apomorphine, sold under the brand name Apokyn among others, is a type of aporphine having activity as a non-selective dopamine agonist which activates both D 2-like and, to a much lesser extent, D 1-like receptors. [2] It also acts as an antagonist of 5-HT 2 and α-adrenergic receptors with high affinity.
Non-selective dopamine receptor agonists include dopamine, deoxyepinephrine (epinine), dinoxyline, and dopexamine. They are mostly peripherally selective drugs , are often also adrenergic receptor agonists , and are used to treat certain cardiovascular conditions .
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS) and are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling.
By 2014, still no selective DRAs had been identified, despite approximately 1,400 compounds having been screened. [7] [3] Similarly, while moderately selective norepinephrine releasing agents (NRAs) are known (e.g., ~10- to 20-fold preference or norepinephrine over dopamine release), [8] [9] [14] [15] no highly selective NRAs had been ...
α-Methyltryptamine [αMT] (Indopan) – non-selective serotonin receptor agonist, serotonin–norepinephrine–dopamine releasing agent (SNDRA), and weak RIMA Etryptamine [α-Ethyltryptamine (αET)] (Monase) – non-selective serotonin receptor agonist, SNDRA, and weak RIMA
Eventually, epinine was determined to be a non-selective stimulant of dopamine (DA) receptors, α-, and β-adrenoceptors, with the stimulation of D 2 receptors leading to inhibition of noradrenergic and ganglionic neurotransmission. These studies, conducted using anesthetized animals, were amplified by van Woerkens and co-workers, who compared ...
Rotigotine acts as a non-selective agonist of the dopamine D 1, D 2, D 3, and, to a lesser extent, D 4 and D 5 receptors, with highest affinity for the D 3 receptor. [15] In terms of affinity, rotigotine has 10-fold selectivity for the D 3 receptor over the D 2, D 4, and D 5 receptors and 100-fold selectivity for the D 3 receptor over the D 1 ...