73029-73-9

Usage

Uses

Used in Pharmaceutical Applications:
CyPPA is used as a positive SK3/SK2 modulator for its ability to reduce the activity of dopaminergic neurons, inhibit dopamine release, and counteract hyperdopaminergic behaviors induced by methyl phenidate. This makes it a potential candidate for the treatment of neurological disorders associated with dopamine dysregulation.
Used in Melanogenesis Inhibition:
CyPPA has been utilized to test its inhibitory functionality on melanogenesis, the process responsible for the production of melanin, the pigment responsible for skin color. Its potential use in this area could lead to the development of treatments for pigmentation disorders and cosmetic applications.
Used in Vascular Function Research:
As an activator of the small conductance potassium channel-3 (SK3), CyPPA has been used in mesenteric artery segments to study its effects on vascular function. This application can provide insights into the role of SK3 channels in blood vessel physiology and contribute to the development of therapies for cardiovascular diseases.
Used in Neuronal Function Studies:
CyPPA has been employed in the activation of calcium-activated potassium (SK) channels in murine hippocampal neurons HT-22 cells. This application aids in understanding the role of SK channels in neuronal function and could contribute to the development of treatments for neurological conditions involving ion channel dysfunction.

Biological Activity

Activator of small conductance Ca 2+ -activated K + channels that displays selectivity for SK2 and SK3 channels (EC 50 values are 5.6 and 14 μ M for SK3 and SK2 respectively). Displays no activity at SK1 and IK channels.

Biochem/physiol Actions

CyPPA is a positive modulator of small conductance Ca2+-activated K+ channels; selective for SK3 and SK2. CyPPA is a first subtype selective SK channel positive modulator with an EC50 of 5.6 μM and 14 μM, efficacy 90% and 71% for hSK3 and hSK2, respectively. CyPPA is a tool for distinguishing SK2 and SK3 from SK1 and IK; no other agents distinguish these channels.

Upstream product

• 67-51-6 3,5-dimethyl-1H-pyrazole 
• 54093-09-3 (2-chloro-6-methyl-pyrimidine-4-yl)-cyclohexylamine 

Relevant academic research and scientific papers

Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels

Background and purpose: Positive modulators of small conductance Ca 2+-activated K+ channels (SK1, SK2, and SK3) exert hyperpolarizing effects that influence the activity of excitable and non-excitable cells. The prototype compound 1

Pyrazolyl-Pyrimidines as Potassium Channel Modulating Agents and Their Medical Use

This invention relates to novel potassium channel modulating agents, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, in particular respiratory diseases, epilepsy, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, schizophrenia, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, immune suppression or pain.

PYRAZOLYL-PYRIMIDINES AS POTASSIUM CHANNEL MODULATING AGENTS AND THEIR MEDICAL USE

This invention relates to novel potassium channel modulating agents of formul (I) with the definitions of R1-R4, X, Y and n according to claiml, and their use in the preparation of pharmaceutical compositions. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassiu channels, in particular respiratory diseases, epilepsy, convulsions, vascular spasms, coronary artery spasms, renal disorders, polycystic kidney disease, bladder spasms, urinary incontinence, bladder outflow obstruction, irritable bowel syndrome, gastrointestinal dysfunction, secretory diarrhoea, ischaemia, cerebral ischaemia, ischaemic heart disease, angina pectoris, coronary heart disease, traumatic brain injury, psychosis, schizophrenia, anxiety, depression, dementia, memory and attention deficits, Alzheimer's disease, dysmenorrhea, narcolepsy, Reynaud's disease, intermittent claudication, Sjorgren's syndrome, migraine, arrhythmia, hypertension, absence seizures, myotonic muscle dystrophia, xerostomi, diabetes type II, hyperinsulinemia, premature labour, baldness, cancer, immune suppression or pain.