RP 60180 : A novel phenothiazine with high affinity for kappa binding sites and with antinociceptive effects in rodents

Fardin, V.; Plau, B.; Carruette, A.; Guyon, Claude; Bardon, T.; Taurand, G.; Laduron, Pierre M.; Garret, C.

doi:10.1016/0304-3959(90)92520-z

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

1995

2022

Publication Types

Select...

Article2

Other1

Relationship

Self Cite0

Independent3

Authors

Journals

Cited by 3 publications

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Phenothiazine and Derivatives

Taurand¹

2000

Ullmann's Encyclopedia of Industrial Chemistry

View full text Add to dashboard Cite

The article contains sections titled: 1. Introduction 2. Uses and Biological Activity 2.1. Therapeutic Uses 2.2. Biological Activity 2.3. Other Uses 3. Syntheses and Reactions 3.1. Ring Syntheses 3.2. N‐Substituted Phenothiazines 3.3. C‐Substituted Phenothiazines 3.4. Analogues and Miscellaneous Compounds 3.5. Other Chemical Properties of the Phenothiazine Nucleus 4. Physical Properties 5. Toxicology

show abstract

Phenothiazine and Derivatives

Taurand¹

2000

Ullmann's Encyclopedia of Industrial Chemistry

View full text Add to dashboard Cite

show abstract

Electrographic studies of the effects of RP 60180, a novel kappa agonist, on the photosensitive baboon Papio papio

Stutzmann¹,

Valin²,

Böhme³

et al. 1995

Progress in Neuro-Psychopharmacology and Biological Psychiatry

View full text Add to dashboard Cite

The Kappa Opioid Receptor: A Promising Therapeutic Target for Multiple Pathologies

et al. 2022

View full text Add to dashboard Cite

Kappa-opioid receptors (KOR) are widely expressed throughout the central nervous system, where they modulate a range of physiological processes depending on their location, including stress, mood, reward, pain, inflammation, and remyelination. However, clinical use of KOR agonists is limited by adverse effects such as dysphoria, aversion, and sedation. Within the drug-development field KOR agonists have been extensively investigated for the treatment of many centrally mediated nociceptive disorders including pruritis and pain. KOR agonists are potential alternatives to mu-opioid receptor (MOR) agonists for the treatment of pain due to their anti-nociceptive effects, lack of abuse potential, and reduced respiratory depressive effects, however, dysphoric side-effects have limited their widespread clinical use. Other diseases for which KOR agonists hold promising therapeutic potential include pruritis, multiple sclerosis, Alzheimer’s disease, inflammatory diseases, gastrointestinal diseases, cancer, and ischemia. This review highlights recent drug-development efforts targeting KOR, including the development of G-protein–biased ligands, mixed opioid agonists, and peripherally restricted ligands to reduce side-effects. We also highlight the current KOR agonists that are in preclinical development or undergoing clinical trials.

show abstract

RP 60180 : A novel phenothiazine with high affinity for kappa binding sites and with antinociceptive effects in rodents

Cited by 3 publications

References 0 publications

Phenothiazine and Derivatives

Phenothiazine and Derivatives

Electrographic studies of the effects of RP 60180, a novel kappa agonist, on the photosensitive baboon Papio papio

The Kappa Opioid Receptor: A Promising Therapeutic Target for Multiple Pathologies

Contact Info

Product

Resources

About