Search Results - "Gullapalli, Srinivas"
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Regulation of Opioid Receptors by Their Endogenous Opioid Peptides
Published in Cellular and molecular neurobiology (01-07-2021)“…Activation of μ, δ, and κ opioid receptors by endogenous opioid peptides leads to the regulation of many emotional and physiological responses. The three major…”
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GRC-6211, a new oral specific TRPV1 antagonist, decreases bladder overactivity and noxious bladder input in cystitis animal models
Published in The Journal of urology (01-01-2009)“…We evaluated the effects of GRC-6211, an orally active TRPV1 antagonist, on the function and noxious input of naïve and inflamed bladders. In urethane…”
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Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)‑one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists
Published in Journal of medicinal chemistry (22-10-2015)“…We report the design and synthesis of novel 5,6-diarylated pyridin-2(1H)-one derivatives as pharmacophoric PDE10A inhibitors. This highly potent molecular…”
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Abstract 1701: EPL-1410, a novel fused heterocycle based orally active dual inhibitor of IDO1/TDO2, as a potential immune-oncology therapeutic
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Many tumors use tryptophan (Trp)-catabolizing enzymes such as Indoleamine/Tryptophan-2,3-dioxygenases (IDO1/TDO2) to induce an immunosuppressive environment by…”
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Modulation of Opiate-Related Signaling Molecules in Morphine-Dependent Conditioned Behavior: Conditioned Place Preference to Morphine Induces CREB Phosphorylation
Published in Neuropsychopharmacology (New York, N.Y.) (01-03-2010)“…Opiate addiction is a chronic, relapsing behavioral disorder where learned associations that develop between the abused opiate and the environment in which it…”
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Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson’s disease model
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…The synthesis and structure-activity relationship studies of a series of compounds from imidazopyridazinone scaffold as PDE7 inhibitors are disclosed. Potent…”
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Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…The design, synthesis and structure activity relationship studies of a series of compounds from benzo[d]imidazo[5,1-b]thiazole scaffold as phosphodiesterase…”
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Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation
Published in Bioorganic & medicinal chemistry letters (01-05-2012)“…The synthesis and structure–activity relationship studies of isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors are discussed. The pharmacokinetic…”
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Characterization of active and inactive states of CB1 receptor and the differential binding state modulation by cannabinoid agonists, antagonists and inverse agonists
Published in Neuropharmacology (01-06-2010)“…Cannabinoid 1 (CB1) receptors have the ability to change conformation between active (R*) and inactive (R) receptor states. Herein, we further characterize…”
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Role of L-type Ca(2+) channels in pertussis toxin induced antagonism of U50,488H analgesia and hypothermia
Published in Brain research (16-08-2002)“…Previous studies have shown that the kappa-opioid effects are sensitive to pertussis toxin (PTX) and affected by Ca(2+) fluxes. However, the possible…”
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Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II
Published in Bioorganic & medicinal chemistry letters (01-08-2014)“…We report the design and synthesis of novel pyrrolo[3,2-b]quinoline containing heteroarene ethers as PDE10A inhibitors with good to excellent potency,…”
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Regulation of dihydropyridine-sensitive Ca(2+) channels during naloxone-induced opioid supersensitivity in rats
Published in European journal of pharmacology (20-09-2002)“…The Ca(2+) channel blocker, nimodipine, increases the chronic naltrexone-induced supersensitivity to morphine analgesia in mice without affecting the density…”
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Regulation of dihydropyridine-sensitive Ca2+ channels during naloxone-induced opioid supersensitivity in rats
Published in European journal of pharmacology (01-09-2002)Get full text
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Role of L-type Ca 2+ channels in pertussis toxin induced antagonism of U50,488H analgesia and hypothermia
Published in Brain research (2002)“…Previous studies have shown that the κ-opioid effects are sensitive to pertussis toxin (PTX) and affected by Ca 2+ fluxes. However, the possible involvement of…”
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15
Regulation of dihydropyridine-sensitive Ca 2+ channels during naloxone-induced opioid supersensitivity in rats
Published in European journal of pharmacology (2002)“…The Ca 2+ channel blocker, nimodipine, increases the chronic naltrexone-induced supersensitivity to morphine analgesia in mice without affecting the density of…”
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16
Role of L-type Ca2+ channels in pertussis toxin induced antagonism of U50,488H analgesia and hypothermia
Published in Brain research (16-08-2002)“…Previous studies have shown that the Kappa -opioid effects are sensitive to pertussis toxin (PTX) and affected by Ca2+ fluxes. However, the possible…”
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17
Role of Ca 2+ channels on the hypothermic response produced by activation of κ-opioid receptors
Published in Pharmacology, biochemistry and behavior (2002)“…The effect of nimodipine (NIM) and lercanidipine (LER) 1,4-dihydropyridine (DHP) calcium channel blockers (CCBs) on the hypothermic response of selective…”
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Role of L-type Ca2+ channels in attenuated morphine antinociception in streptozotocin-diabetic rats
Published in European journal of pharmacology (25-01-2002)“…The role of L-type Ca2+ channels in morphine antinociception was studied in streptozotocin-induced diabetic and control rats, using [3H]PN200-110 [isopropyl…”
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Role of L-type Ca 2+channels in attenuated morphine antinociception in streptozotocin-diabetic rats
Published in European journal of pharmacology (2002)“…The role of L-type Ca 2+ channels in morphine antinociception was studied in streptozotocin-induced diabetic and control rats, using [ 3H]PN200-110 {isopropyl…”
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Potentiation of κ-opioid receptor agonist-induced analgesia and hypothermia by fluoxetine
Published in Pharmacology, biochemistry and behavior (01-05-2001)“…The effect of fluoxetine, a selective 5-HT reuptake inhibitor on the analgesic and hypothermic response of trans-(±)-3,4-dichloro- N-methyl-…”
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