Search Results - "Bhyrapuneni, Gopinadh"

Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation by Nirogi, Ramakrishna, Benade, Vijay, Daripelli, Saivishal, Subramanian, Ramkumar, Kamuju, Venkatesh, Bhyrapuneni, Gopinadh, Muddana, Nageswara Rao, Mekala, Venkat Reddy, Petlu, Surendra, Jayarajan, Pradeep, Badange, Rajesh, Shinde, Anil, Jasti, Venkat

“…Rationale Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability…”
Get full text

Histamine 3 receptor inverse agonist Samelisant (SUVN-G3031): Pharmacological characterization of an investigational agent for the treatment of cognitive disorders by Nirogi, Ramakrishna, Grandhi, Venkata R, Medapati, Rajesh B, Ganuga, Narender, Benade, Vijay, Gandipudi, Sudhakar, Manoharan, Arunkumar, Abraham, Renny, Jayarajan, Pradeep, Bhyrapuneni, Gopinadh, Shinde, Anil, Badange, Rajesh K, Subramanian, Ramkumar, Petlu, Surendra, Jasti, Venkat

“…Background: Central histamine H3 receptors are a family of presynaptic auto and heteroreceptors. Blockade of the presynaptic H3 receptors activates the…”
Get full text

Inhibition of cytochrome P450 enzymes by saturated and unsaturated fatty acids in human liver microsomes, characterization of enzyme kinetics in the presence of bovine serum albumin (0.1 and 1.0% w/v) and in vitro – in vivo extrapolation of hepatic clearance by Palacharla, Raghava Choudary, Uthukam, Venkatesham, Manoharan, Arunkumar, Ponnamaneni, Ranjith Kumar, Padala, Nagasurya Prakash, Boggavarapu, Rajesh Kumar, Bhyrapuneni, Gopinadh, Ajjala, Devender Reddy, Nirogi, Ramakrishna

“…The objective of the study was to determine the effect of fatty acids on CYP enzymes and the effect of BSA on intrinsic clearance of probe substrates. The…”
Get full text

Chemical inhibitors of CYP450 enzymes in liver microsomes: combining selectivity and unbound fractions to guide selection of appropriate concentration in phenotyping assays by Nirogi, Ramakrishna, Palacharla, Raghava Choudary, Uthukam, Venkatesham, Manoharan, Arunkumar, Srikakolapu, Surya Rao, Kalaikadhiban, Ilayaraja, Boggavarapu, Rajesh Kumar, Ponnamaneni, Ranjith Kumar, Ajjala, Devender Reddy, Bhyrapuneni, Gopinadh

“…Abstract 1. Chemical inhibition is the widely used method in reaction phenotyping assays for estimation of specific enzyme contribution to a given metabolic…”
Get full text

Identification of a suitable and selective inhibitor towards aldehyde oxidase catalyzed reactions by Nirogi, Ramakrishna, Kandikere, Vishwottam, Palacharla, Raghava Choudary, Bhyrapuneni, Gopinadh, Kanamarlapudi, Vijaya Bhargava, Ponnamaneni, Ranjith Kumar, Manoharan, Arun Kumar

“…Abstract 1. Aldehyde oxidase (AO) is a liver cytosolic molybdoflavoprotein enzyme whose importance in drug metabolism is gaining in the recent. The objective…”
Get full text

Rat thalamic α4β2 neuronal nicotinic acetylcholine receptor occupancy assay using LC–MS/MS by Nirogi, Ramakrishna, Kandikere, Vishwottam, Bhyrapuneni, Gopinadh, Saralaya, Ramanatha, Muddana, Nageswararao, Ajjala, Devender Reddy

“…In vivo brain receptor occupancy has been the key assay in driving preclinical drug discovery program and there is a need to hasten this screening step…”
Get full text

Evaluation of monoamine oxidase A and B type enzyme occupancy using non-radiolabelled tracers in rat brain by Thentu, Jagadeesh Babu, Bhyrapuneni, Gopinadh, Padala, Nagasurya Prakash, Chunduru, Prathyusha, Pantangi, Hanumanth Rao, Nirogi, Ramakrishna

“…Monoamine oxidase (MAO) enzymes, type A and B metabolise the amine neurotransmitters of the body. Selective inhibition of either enzyme is an approach for…”
Get full text

506 Samelisant: Baseline Characteristics from a Phase 2 Study Evaluating Efficacy and Safety in Patients with Narcolepsy by Nirogi, Ramakrishna, Ravula, Jyothsna, Jayarajan, Pradeep, Jetta, Satish, Bhyrapuneni, Gopinadh, Benade, Vijay, Shinde, Anil, Goyal, Vinod

“…Abstract Introduction histamine H3 receptor (H3R) antagonists/ inverse agonists increase histaminergic neurotransmission and offer a therapeutic option for the…”
Get full text

The use of inactivated brain homogenate to determine the in vitro fraction unbound in brain for unstable compounds by Nirogi, Ramakrishna, Molgara, Parusharamulu, Bhyrapuneni, Gopinadh, Manoharan, Arunkumar, Padala, Nagasurya Prakash, Palacharla, Veera Raghava Chowdary

“…The use of IBH-5 decreased the k deg values and increased the half-life of the compounds PNZ, TCP, Cpd I and Cpd II with k deg values of 1.10 × 10 −4  s − 1 (t…”
Get full text

A simple and rapid method to collect the cerebrospinal fluid of rats and its application for the assessment of drug penetration into the central nervous system by Nirogi, Ramakrishna, Kandikere, Vishwottam, Mudigonda, Koteshwara, Bhyrapuneni, Gopinadh, Muddana, Nageswararao, Saralaya, Ramanatha, Benade, Vijay

“…Many central nervous system (CNS) drug discovery programs require the successful collection of cerebrospinal fluid (CSF) for assessing CNS penetration and…”
Get full text

Development and Validation of a Higher-Throughput Cytochrome P450 Inhibition Assay with the Novel Cofactor-Supplemented Permeabilized Cryopreserved Human Hepatocytes (MetMax Human Hepatocytes) by Palacharla, Veera Raghava Choudary, Chunduru, Prathyusha, Ajjala, Devender Reddy, Bhyrapuneni, Gopinadh, Nirogi, Ramakrishna, Li, Albert P

“…Here, we report the application of a novel hepatocyte system, the cofactor-supplemented permeabilized cryopreserved human hepatocytes [MetMax human hepatocytes…”
Get full text

A sensitive and selective quantification of catecholamine neurotransmitters in rat microdialysates by pre-column dansyl chloride derivatization using liquid chromatography–tandem mass spectrometry by Nirogi, Ramakrishna, Komarneni, Prashanth, Kandikere, Vishwottam, Boggavarapu, Rajeshkumar, Bhyrapuneni, Gopinadh, Benade, Vijay, Gorentla, Srinivasarao

“…► Dansyl chloride derivatization of dopamine and norepinephrine in rat microdialysates. ► Sensitive and selective method to determine the basal levels in rat…”
Get full text

0139 SUVN-G3031, A Potent and Selective Histamine H3 Receptor Inverse Agonist - Phase-2 Investigational New Drug for the Treatment of Narcolepsy - Differentiating Factors with Competitor Clinical Candidates by Nirogi, Ramakrishna, Bhyrapuneni, Gopinadh, Abraham, Renny, Subramanian, Ramkumar, Goyal, Vinod Kumar, Pandey, Santosh Kumar, Badange, Rajesh, Shinde, Anil

“…Introduction SUVN-G3031 is one of the potent H3 receptor (H3R) inverse agonist in the clinical development for the treatment of narcolepsy with or without…”
Get full text

Masupirdine in combination with donepezil and memantine in patients with moderate Alzheimer's disease: Subgroup analyses of memantine regimen, plasma concentrations and duration of treatment: Human/Human trials: Other by Nirogi, Ramakrishna, Goyal, Vinod Kumar, Bhyrapuneni, Gopinadh, Palacharla, Veera Raghava Chowdary, Ravulu, Jyothsna, Jetta, Satish, Jasti, Venkat

“…Abstract Background Masupirdine (SUVN‐502), a selective 5‐hydroxytryptamine‐6 (5‐HT 6 ) receptor antagonist has demonstrated efficacy in animal models of…”
Get full text

Masupirdine in combination with donepezil and memantine in patients with moderate Alzheimer's disease: Subgroup analyses of memantine regimen, plasma concentrations and duration of treatment by Nirogi, Ramakrishna, Goyal, Vinod Kumar, Bhyrapuneni, Gopinadh, Palacharla, Veera Raghava Chowdary, Ravulu, Jyothsna, Jetta, Satish, Jasti, Venkat

“…Background Masupirdine (SUVN‐502), a selective 5‐hydroxytryptamine‐6 (5‐HT6) receptor antagonist has demonstrated efficacy in animal models of cognitive…”
Get full text

SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization by Nirogi, Ramakrishna, Abraham, Renny, Benade, Vijay, Medapati, Rajesh B, Jayarajan, Pradeep, Bhyrapuneni, Gopinadh, Muddana, NageswaraRao, Mekala, Venkat R, Subramanian, Ramkumar, Shinde, Anil, Kambhampati, Ramasastry, Jasti, Venkat

“…Research in Alzheimer’s disease is going through a big turnaround. New palliative therapies are being reconsidered for the effective management of disease…”
Get full text

Masupirdine (SUVN‐502): A promising clinical candidate for the management of agitation in Alzheimer’s dementia by Nirogi, Ramakrishna, Jayarajan, Pradeep, Tadiparthi, Jayaprakash, Shinde, Anil K, Rasheed, Mohammed Abdul, Goyal, Vinod Kumar, Bhyrapuneni, Gopinadh, Benade, Vijay, Palacharla, Veera Raghava Chowdary, Ravula, Jyothsna, Jetta, Satish

“…Background Masupirdine is a potent and selective 5‐HT6 receptor antagonist and has completed Phase‐2 clinical proof of concept studies in patients with…”
Get full text

SUVN‐D4010: A serotonin‐4 receptor partial agonist for the treatment of cognitive disorders by Medapati, Rajesh Babu, Ganuga, Narender, Mekala, Venkat Reddy, Bhyrapuneni, Gopinadh, Thentu, Jagadeesh Babu, Daripelli, Saivishal, Gagginapalli, Shankar Reddy, Bogaraju, Narsimha, Rasheed, Mohammed Abdul, Nirogi, Ramakrishna

“…Background Memory impairments are clinical symptoms of a wide range of neurodegenerative diseases, and natural physiological process such as ageing. SUVN‐D4010…”
Get full text

SUVN-502 + DONEPEZIL + MEMANTINE (TRIPLE COMBINATION): FIRST-IN-CLASS AND A PROMISING NEW APPROACH FOR THE SYMPTOMATIC TREATMENT OF ALZHEIMER'S DISEASE DEMENTIA by Jayarajan, Pradeep, Bhyrapuneni, Gopinadh, Benade, Vijay, Fernandes, Joylee, Kommineni, Santi Sree, Nirogi, Ramakrishna, Jasti, Venkat

Get full text

P1‐089: SUVN‐502 + DONEPEZIL + MEMANTINE (TRIPLE COMBINATION): FIRST‐IN‐CLASS AND A PROMISING NEW APPROACH FOR THE SYMPTOMATIC TREATMENT OF ALZHEIMER'S DISEASE DEMENTIA by Jayarajan, Pradeep, Bhyrapuneni, Gopinadh, Benade, Vijay, Fernandes, Joylee, Kommineni, Santi Sree, Nirogi, Ramakrishna, Jasti, Venkat

Get full text