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Receptor kappa

Mansour A, Fox C, Meng F, Akil H, Watson S. Kappa 1 receptor mRNA in the rat CNS comparison of kappa receptor binding and prodynorphin mRNA. Mol Cell Neurosci 1994 5 124-144. [Pg.483]

OTHER REVIEWS OF THE OPIOID LITERATURE INTRODUCTION SELECTIVE KAPPA OPIOID LIGANDS KAPPA RECEPTOR SUBTYPES... [Pg.109]

A comprehensive review of receptor selective opioid peptide analogues by Schiller [7] appeared in the previous volume of this Series and for this reason the present chapter describes only non-peptide structures. A leading review which introduces kappa opioid analgesics was written by Horwell in 1988 [8] and a subsequent article focusing on kappa receptors and analgesia by Millan appeared in 1990 [9]. [Pg.111]

The biochemical and pharmacological properties of the kappa receptor and the differences between the kappa, mu and delta receptors have been reviewed elsewhere. The reader is directed to the opioid review articles by Rees and Hunter (1990) [4], Casy (1989) [3] and Leslie (1987) [10] and also to two shorter reviews which deal specifically with kappa agonists the review by Horwell published in 1988 entitled Kappa Opioid Analgesics [8] and the review by Millan in 1990 on kappa opioid receptors and analgesia [9]. An account of the medicinal chemistry of selective opioid agonists and antagonists was published in 1990 by Zimmerman and Leander [5]. [Pg.113]

As discussed above, the discovery by the Upjohn Company in 1982 of U-50488 (5) was a milestone achievement in opioid research. This compound has significantly greater selectivity for the kappa opioid receptor than the previously used ketazocine (2) or EKC (3) and its widespread use in opioid research to study the properties of the kappa receptor has led to its being generally regarded as the prototype non-peptide kappa selective agonist. [Pg.116]

Attaching an isothiocyanate group to the aromatic ring of U-50488 has been reported to produce the first site-directed alkylating agent to bind irreversibly to kappa receptors in guinea-pig membranes [51]. [Pg.119]

Mu and kappa receptor agonists have been shown to affect central dopaminergic activity in rodents in vivo and in vitro [78, 79]. This has been investigated with RP 60180 (51), which decreases dopamine (DA) utilization in rat prefrontal cortex and in the striatum (by 30—35 % and 10 % respectively at 1-2.5 mg/kg s.c.) whereas the mu agonist morphine causes a significant increase (90-150% and 30 40% respectively at 5 mg/kg), an effect which is abolished by RP 60180 (1 2.5 mg/kg) [80]. [Pg.127]

The 1,2-aminoamides are now established as a chemical series with several highly selective kappa opioid receptor agonists. However, the biological activity of 1,2-aminoamides is not restricted to kappa analgesics. Several related structures exhibit biological activity in other systems of importance and interest. In order to appraise the significance of this chemical class and to put the SAR for kappa receptor activity into context, a selection of these compounds is discussed here. This is not a comprehensive literature review but rather a selection of a few compounds to illustrate the broad range of medieinal activity exhibited by these somewhat similar chemical structures. [Pg.127]

In the above discussion on the mu/kappa receptor selectivity of the U-50488 (5) series, the steric properties of the tertiary amine and the distance between the amide and the aromatic ring were cited as important factors. This has been exploited by the Upjohn company to give the arylformamide-dimethyl-amine derivative (52) which is an analgesic in the mouse tail flick test (ED50 = 0.2 mg/kg s.c.) and causes mu-opioid like side-effects such as Straub tail, arched back and increased locomotor activity [81]. These behavioural effects and the association constant for the morphine receptor of compound... [Pg.127]

The majority of studies aimed at preparing kappa-selective opioids have used U-50488 (5) as the chemical lead and, as the above discussion shows, this has proved to be a highly productive approach. However, as was pointed out above, there are other structures [EKC (3), tifluadom (6) and the peptide dynorphin (7)] which have been reported to bind to the kappa receptor, albeit with poor opioid receptor subtype selectivity. Some attempts have been made to develop kappa-selective ligands from these structures and they are summarized here. [Pg.130]

The plant alkaloids mimic the endogenous peptides enkephalins and endorphins (Chapter 12), which meditate nociception and sleep. There are three types of widely distributed opiate receptors. Mu receptors are concentrated in neocortex, striatum, thalamus, hippocampus, amygdala and spinal cord, delta receptors in neocortex and amydala, and kappa receptors in striatum, amygdala and hypothalamus (Mansour et al., 1988). [Pg.218]

Opioid receptors are found in the dorsal horn as well as in other areas throughout the spinal cord and brain. Three major classes of opioid receptors exist mu receptors (/r), kappa receptors (k) and delta... [Pg.435]

Delta and kappa receptors can also contribute to analgesia, particularly at spinal level. Although morphine also acts on kappa and delta sites but it is not clear that up to what level they contribute in its analgesic action. [Pg.76]

It is a strong kappa receptor agonist and mu receptor antagonist. Its agonistic property is approximately three to four times more than pentazocine and its antagonistic property is approximately 10 times more than pentazocine. It has less abuse liability in comparison to pentazocine. It is useful in postoperative pain, myocardial infarction and labour. [Pg.80]

Scopes, D.I. Recent developments in non-peptide kappa receptor agonists, Drug Fut. 1993, 18, 933-947. [Pg.149]

Dooley, C. and Houghten, R. (Torrey Pines Institute for Molecular Studies) Novel kappa receptor selective opioid peptides, W09640206 (1996), US5610271 (1997). [Pg.157]

Mu receptors are almost always located proximally, on the presynaptic side of the synapse. The periaqueductal gray is the region containing the most mu receptors, but they are also found in the superficial dorsal hom of the spinal cord, the external plexiform layer of the olfactory bulb, the nucleus accumbens (an area deeply implicated in the process of addiction), in some parts of the cerebral cortex, and in some of the nuclei of the amygdala. Mu receptors avidly bind enkephalins and beta-endorphin, but they have a low affinity for dynorphins (primarily a kappa receptor agonist).6... [Pg.50]

Activation of kappa receptors also produces analgesia, but it simultaneously induces nausea and dysphoria. Kappa receptors are located mainly on pain neurons located in the spinal cord and, to a lesser extent in the brain. They bind to an endogenously occurring ligand called dynorphin. [Pg.50]

Table 8.1 shows a selective timeline of the evaluation, abuse, and regulation of butorphanol, an opioid with mixed activity at mu and kappa receptors. The most salient aspects of the drug s recent history can be summed up in terms of two questions ... [Pg.153]


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Kappa

Kappa opioid receptor agonist

Kappa receptor agonists

Kappa receptors activation

Kappa receptors affecting

Kappa receptors agonist-antagonists/partial agonists

Kappa receptors cloning

Kappa receptors morphine

Kappa receptors pain modulation

Kappa-opioid receptor activation

Kappa-opioid receptors

Kappa-selective opioid receptor

Kappa-selective opioid receptor agonists

Kappa-selective opioid receptor antagonists

Opiate receptors kappa

Opioid analgesics kappa-receptor selective

Opioid receptor kappa sigma

Opioids kappa receptor

Receptors) kappa analgesic

Regulation kappa-opioid receptors

The kappa receptor (k)

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