Sigma receptor (σR) ligands with antiproliferative and anticancer activity

MO Georgiadis, O Karoutzou, AS Foscolos… - Molecules, 2017 - mdpi.com
Sigma receptor (σR) ligands have proven to be useful as cancer diagnostics and anticancer
therapeutics and their ligands have been developed as molecular probes in oncology …

Sigma receptor modulators: a patent review

S Collina, R Gaggeri, A Marra, A Bassi… - Expert opinion on …, 2013 - Taylor & Francis
Introduction: Sigma receptors are involved in several central nervous system (CNS)
disorders, including mood disorders (depression and anxiety), psychosis, schizophrenia …

Structural features important for. sigma. 1 receptor binding

RA Glennon, SY Ablordeppey, AM Ismaiel… - Journal of medicinal …, 1994 - ACS Publications
Two problems that have hampered a receptor research are (i) a lack of high-affinity agents
and (ii) the recent identification of multiple populations of a receptors (ie, a\and< 72 sites) …

Sigma receptor ligands and the use thereof

RA Glennon - US Patent 6,057,371, 2000 - Google Patents
The invention relates to methods for the treatment of central nervous system disorders,
gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by …

Monoamine oxidase inhibitory properties of some methoxylated and alkylthio amphetamine derivatives: structure–activity relationships

MC Scorza, C Carrau, R Silveira… - Biochemical …, 1997 - Elsevier
The monoamine oxidase (MAO) inhibitory properties of a series of amphetamine derivatives
with different substituents at or around the para position of the aromatic ring were evaluated …

Enantiomeric N-substituted N-normetazocines: a comparative study of affinities at. sigma., PCP, and. mu. opioid receptors

FI Carroll, P Abraham, K Parham, X Bai… - Journal of medicinal …, 1992 - ACS Publications
The optical antipodes of iV-allyl-N-normetazocine (2; SKF 10047, NANM) were the original
compounds used for the classification of the a receptor as distinct from otherreceptors such …

. sigma. Ligands with Subnanomolar Affinity and Preference for the. sigma. 2 Binding Site. 2. Spiro-Joined Benzofuran, Isobenzofuran, and Benzopyran Piperidines

EK Moltzen, J Perregaard, E Meier - Journal of Medicinal …, 1995 - ACS Publications
(01)= 1.5 nM, 1050 (02)= 0.07 nM). Introduction of substituents in the benzene ring of the
spiro [isobenzofuran-l (3iT), 4'-piperidine] ring system of Lu 28-179 mainly affects affinity for …

Early development of sigma-receptor ligands

S Narayanan, R Bhat, C Mesangeau… - Future medicinal …, 2011 - Taylor & Francis
Sigma receptors (σ-1 and σ-2) are non-opioid proteins implicated in the pathophysiology of
various neurological disorders and cancer. The σ-1 subtype is a chaperon protein widely …

Sigma receptor ligands and the use thereof

RA Glennon, JB Fischer - US Patent 6,087,346, 2000 - Google Patents
The invention relates to methods for the treatment of central nervous system disorders,
neurological disorders, gas trointestinal disorders, drug abuse, angina, migraine, hyper …

Synthesis, structure and quantitative structure-activity relationships of σ receptor ligands, 1-[2-(3, 4-dimethoxyphenyl) ethyl]-4-(3-phenylpropyl) piperazines

K Fujimura, J Matsumoto, M Niwa, T Kobayashi… - Bioorganic & Medicinal …, 1997 - Elsevier
A set of the title compounds having different substituents (R1, R2) on their phenyl groups
was synthesized to find σ receptor binding affinity. Among the compounds, 2b (R1 R2 Cl) …