| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Kevin M Braunscheidel, George Voren, Christie D Fowler, Qun Lu, Alexander Kuryatov, Michael D Cameron, Ines Ibañez-Tallon, Jon M Lindstrom, Theodore M Kamenecka, Paul J Kenn. SR9883 is a novel small-molecule enhancer of α4β2* nicotinic acetylcholine receptor signaling that decreases intravenous nicotine self-administration in rats. Frontiers in molecular neuroscience. vol 17. 2024-09-30. PMID:39346680. |
evidence suggests that positive allosteric modulators (pam) and other enhancers of nicotinic acetylcholine receptor (nachr) signaling could have therapeutic utility as smoking cessation agents. |
2024-09-30 |
2024-10-02 |
rat |
| Sami Alzarea, Muzaffar Abbas, Patrick J Ronan, Kabirullah Lutfy, Shafiqur Rahma. The Effect of an α-7 Nicotinic Allosteric Modulator PNU120596 and NMDA Receptor Antagonist Memantine on Depressive-like Behavior Induced by LPS in Mice: The Involvement of Brain Microglia. Brain sciences. vol 12. issue 11. 2022-11-11. PMID:36358419. |
in the present study, we assessed the effects of pnu120596, an α7 nachr positive allosteric modulator (pam), on haao expression and quin formation in the hippocampus and prefrontal cortex. |
2022-11-11 |
2023-08-14 |
mouse |
| Sami Alzarea, Muzaffar Abbas, Patrick J Ronan, Kabirullah Lutfy, Shafiqur Rahma. The Effect of an α-7 Nicotinic Allosteric Modulator PNU120596 and NMDA Receptor Antagonist Memantine on Depressive-like Behavior Induced by LPS in Mice: The Involvement of Brain Microglia. Brain sciences. vol 12. issue 11. 2022-11-11. PMID:36358419. |
therefore, α7 nachr pam could be a potential therapeutic candidate for mdd associated with neurotoxic glutamatergic transmission. |
2022-11-11 |
2023-08-14 |
mouse |
| Roger L Papke, Madison Karaffa, Nicole A Horenstein, Clare Stoke. Coffee and cigarettes: Modulation of high and low sensitivity α4β2 nicotinic acetylcholine receptors by n-MP, a biomarker of coffee consumption. Neuropharmacology. 2022-06-30. PMID:35772522. |
when co-applied with pnu-120596, a positive allosteric modulator (pam), the coffees stimulated currents from cells expressing α7 nachr that were larger than ach controls. |
2022-06-30 |
2023-08-14 |
human |
| Muzaffar Abbas, Sami Alzarea, Roger L Papke, Shafiqur Rahma. Effects of α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator on BDNF, NKCC1 and KCC2 Expression in the Hippocampus following Lipopolysaccharide-Induced Allodynia and Hyperalgesia in a Mouse Model of Inflammatory Pain. CNS & neurological disorders drug targets. vol 20. issue 4. 2021-12-01. PMID:33380307. |
the effects of 3a,4,5,9b-tetrahydro-4-(1-naphthalenyl)-3h-cyclopentan[c]quinoline-8-sulfonamide (tqs), an α7 nicotinic acetylcholine receptor positive allosteric modulator (nachr pam), on hippocampal bdnf, cation-chloride cotransporters, nkcc1 and kcc2, expression in inflammatory pain are not known. |
2021-12-01 |
2023-08-13 |
mouse |
| Gokhan Unal, Serap Sirvanci, Feyza Ariciogl. α7 nicotinic receptor agonist and positive allosteric modulators differently improved schizophrenia-like cognitive deficits in male rats. Behavioural brain research. vol 397. 2021-11-15. PMID:33011186. |
this study comparatively investigated the effect of α7 nachr agonist (a-582941), type i pam (ccmi), type ii pam (pnu-120596), and the antipsychotic drug (clozapine) on behavioral, molecular, and immunohistochemical parameters in a subchronic mk-801 model of schizophrenia in male rats. |
2021-11-15 |
2023-08-13 |
human |
| Britta Hahn, Carolyn H Reneski, Malcom Lane, Greg I Elmer, Edna F R Pereir. Evidence for positive allosteric modulation of cognitive-enhancing effects of nicotine by low-dose galantamine in rats. Pharmacology, biochemistry, and behavior. vol 199. 2021-07-07. PMID:33022302. |
the co-administration of a nachr positive allosteric modulator (pam) may enable larger effects by potentiating nachr responses to an agonist. |
2021-07-07 |
2023-08-13 |
rat |
| Britta Hahn, Carolyn H Reneski, Malcom Lane, Greg I Elmer, Edna F R Pereir. Evidence for positive allosteric modulation of cognitive-enhancing effects of nicotine by low-dose galantamine in rats. Pharmacology, biochemistry, and behavior. vol 199. 2021-07-07. PMID:33022302. |
the acetylcholinesterase (ache) inhibitor galantamine is a nachr pam at a low dose range. |
2021-07-07 |
2023-08-13 |
rat |
| Britta Hahn, Carolyn H Reneski, Malcom Lane, Greg I Elmer, Edna F R Pereir. Evidence for positive allosteric modulation of cognitive-enhancing effects of nicotine by low-dose galantamine in rats. Pharmacology, biochemistry, and behavior. vol 199. 2021-07-07. PMID:33022302. |
furthermore, these findings provide a general proof-of-principle for a nachr agonist and pam combination strategy for cognitive enhancement. |
2021-07-07 |
2023-08-13 |
rat |
| Ali Yehia, Haiyang We. Studying Nicotinic Acetylcholine Receptors Using the IonFlux™ Microfluidic-Based Automated Patch-Clamp System with Continuous Perfusion and Fast Solution Exchange. Current protocols in pharmacology. vol 88. issue 1. 2021-07-01. PMID:32068960. |
we present protocols to study agonist, antagonist, and pam activities on nachrs, particularly the rapidly desensitizing nachr α7 receptors. |
2021-07-01 |
2023-08-13 |
Not clear |
| Hui Li, Jie Gao, Yue Chang, Kexin Li, Lei Wang, Chuanxia Ju, Fang Zhan. JWX-A0108, a positive allosteric modulator of α7 nAChR, attenuates cognitive deficits in APP/PS1 mice by suppressing NF-κB-mediated inflammation. International immunopharmacology. vol 96. 2021-06-22. PMID:33975230. |
jwx-a0108 is a type i positive allosteric modulator (pam) of α7 nachr, which mainly enhances agonist-evoked peak currents. |
2021-06-22 |
2023-08-13 |
mouse |
| Ayman K Hamouda, Malia R Bautista, Lois S Akinola, Yasmin Alkhlaif, Asti Jackson, Moriah Carper, Wisam B Toma, Sumanta Garai, Yen-Chu Chen, Ganesh A Thakur, Christie D Fowler, M Imad Dama. Potentiation of (α4)2(β2)3, but not (α4)3(β2)2, nicotinic acetylcholine receptors reduces nicotine self-administration and withdrawal symptoms. Neuropharmacology. vol 190. 2021-06-09. PMID:33878302. |
we utilized two nachr positive allosteric modulators (pams): desformylflustrabromine (dfbr), a pam of both the ls and hs α4β2 nachrs, and cmpi, a pam selective for the ls nachr. |
2021-06-09 |
2023-08-13 |
mouse |
| Mahip K Verma, Rajan N Goel, Anand M Bokare, Manoj P Dandekar, Sarita Koul, Sagar Desai, Santoshkumar Tota, Nilendra Singh, Prashant B Nigade, Vinod B Patil, Dipak Modi, Maneesh Mehta, Jayasagar Gundu, Sameer S Walunj, Navnath P Karche, Neelima Sinha, Rajender K Kamboj, Venkata P Pall. LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization. European journal of pharmacology. vol 891. 2021-05-20. PMID:33127363. |
positive allosteric modulation (pam) of α7 nachr represents an innovative approach to amplify endogenous cholinergic signaling in a temporally restricted manner in learning and memory centers of brain. |
2021-05-20 |
2023-08-13 |
Not clear |
| Mahip K Verma, Rajan N Goel, Anand M Bokare, Manoj P Dandekar, Sarita Koul, Sagar Desai, Santoshkumar Tota, Nilendra Singh, Prashant B Nigade, Vinod B Patil, Dipak Modi, Maneesh Mehta, Jayasagar Gundu, Sameer S Walunj, Navnath P Karche, Neelima Sinha, Rajender K Kamboj, Venkata P Pall. LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization. European journal of pharmacology. vol 891. 2021-05-20. PMID:33127363. |
here we describe a novel α7 nachr pam, ll-00066471, which potently amplified agonist-induced ca |
2021-05-20 |
2023-08-13 |
Not clear |
| István Ledneczki, Pál Tapolcsányi, Eszter Gábor, András Visegrády, Márton Vass, János Éles, Patrik Holm, Anita Horváth, Anikó Pocsai, Sándor Mahó, István Greiner, Balázs Krámos, Zoltán Béni, János Kóti, Anna E Káncz, Márta Thán, Sándor Kolok, Judit Laszy, Ottilia Balázs, Gyula Bugovits, József Nagy, Mónika Vastag, Ágota Szájli, Éva Bozó, György Lévay, Balázs Lendvai, Zsolt Németh. Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach. European journal of medicinal chemistry. vol 214. 2021-04-30. PMID:33540354. |
the paper focuses on the scaffold hopping-based discovery and characterization of novel nicotinic alpha 7 receptor positive modulator (α7 nachr pam) ligands around the reference molecule (a-867744). |
2021-04-30 |
2023-08-13 |
mouse |
| Junsuke Uwada, Hitomi Nakazawa, Daisuke Mikami, Mohammad Sayful Islam, Ikunobu Muramatsu, Takanobu Taniguchi, Takashi Yazaw. PNU-120596, a positive allosteric modulator of α7 nicotinic acetylcholine receptor, directly inhibits p38 MAPK. Biochemical pharmacology. vol 182. 2021-01-21. PMID:33132165. |
pnu-120596 is a classical positive allosteric modulator (pam) of α7 nicotinic acetylcholine receptor (α7 nachr) and widely used to investigate the effect of α7 nachr activation on several inflammation-associated diseases including rheumatoid arthritis, inflammatory bowel disease and cerebral ischemia. |
2021-01-21 |
2023-08-13 |
Not clear |
| Zsolt Kristóf Bali, Lili Veronika Nagy, Dénes Budai, István Hernád. Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Scientific reports. vol 9. issue 1. 2020-10-26. PMID:31249369. |
the simultaneous application of alpha7 nachr agonist pha-543613 and pam ns-1738 resulted in additive increase of both spontaneous and nmda-evoked firing rate. |
2020-10-26 |
2023-08-13 |
rat |
| Krisztina Pesti, Peter Lukacs, Arpad Mik. Type I-like behavior of the type II α7 nicotinic acetylcholine receptor positive allosteric modulator A-867744. PeerJ. vol 7. 2020-09-30. PMID:31534841. |
our results emphasize that subtle details of the mechanism of action may be significant in assessing the therapeutic applicability of α7 nachr pam compounds. |
2020-09-30 |
2023-08-13 |
Not clear |
| Marloes van Hout, Jessica Klein, Philip K Ahring, David T Brown, Siganya Thaneshwaran, Altair B Dos Santos, Anders A Jensen, Kristi A Kohlmeier, Palle Christophersen, Tino Dyhrin. Characterization of AN6001, a positive allosteric modulator of α6β2-containing nicotinic acetylcholine receptors. Biochemical pharmacology. vol 174. 2020-08-24. PMID:31887290. |
here, we report the discovery and characterization of an6001, a novel selective α6β2* nachr pam. |
2020-08-24 |
2023-08-13 |
human |
| Neelima Sinha, Navnath P Karche, Mahip Kalyan Verma, Sameer S Walunj, Prashant B Nigade, Gourhari Jana, Sanjay P Kurhade, Anil K Hajare, Ajay R Tilekar, Ganesh R Jadhav, Baban R Thube, Javed S Shaikh, Sudhakar Balgude, Lairikyengbam Bikramjit Singh, Vijaya Mahimane, Shridhar K Adurkar, Girish Hatnapure, Firoj Raje, Yogesh Bhosale, Dnyaneshwar Bhanage, Sachchidanand Sachchidanand, Ruchi Dixit, Rajesh Gupta, Anand M Bokare, Manoj Dandekar, Ashish Bharne, Manavi Chatterjee, Sagar Desai, Sarita Koul, Dipak Modi, Maneesh Mehta, Vinod Patil, Minakshi Singh, Jayasagar Gundu, Rajan N Goel, Chirag Shah, Sharad Sharma, Dhananjay Bakhle, Rajender Kumar Kamboj, Venkata P Pall. Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization. Journal of medicinal chemistry. vol 63. issue 3. 2020-08-03. PMID:31755711. |
the discovery of a series of thiophenephenylsulfonamides as positive allosteric modulators (pam) of α7 nicotinic acetylcholine receptor (α7 nachr) is described. |
2020-08-03 |
2023-08-13 |
Not clear |