Friday, February 16, 2018 9:14:19 AM
Sertraline (SSRI) 31.6
Fluoxetine (SSRI) 191.2
Escitalopram (SSRI) 288.3
Citalopram (SSRI) 403.8
Paroxetine (SSRI) 2041
Duoxetine (SNRI) 3533
Venlafaxine (SNRI) >10,000 Milnacipran (SNRI) >10,000 Mirtazapine (NaSSA) >10,000
Activation of sigma-1 receptor chaperone in the treatment of neuropsychiatric diseases and its clinical implication
https://ac.els-cdn.com/S1347861314000176/1-s2.0-S1347861314000176-main.pdf?_tid=188f1d70-1319-11e8-a85c-00000aab0f01&acdnat=1518786094_9ee528a53583943bed94a71e95778fce
· Donepezil (Aricept®) is a potent acetylcholinesterase inhibitor that is used in treating Alzheimer's disease. The compound is also a potent sigma-1 receptor ligand with an affinity of 14.6 nM
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2785038/
The receptor binding profile of Anavex 2-73 is:
Ki of 860 nM for sigma 1 receptor
https://investorshub.advfn.com/boards/read_msg.aspx?message_id=118560971
Probably a decent idea to read the above link imho.
“Usually, the *lower* the Ki number, the more affinity; which is measured by the displacement of another (radiolabled for example) exogenous ligand.”
“For binding affinity people generally are referring to either the dissociation constant (the Kd value) or the association constant, Ka, which has no units. For your question why does it seem backwards, well Ka = 1/Kd. If units are given it is usually referring to Kd, the equilibrium dissociation constant (equilibrium referring to the binding and unbinding reactions).
Ki, or the inhibition constant, has to do with competitive binding assays and relates the ligand with the amount of competitor that displaces half of it (the IC50). “
http://www.bluelight.org/vb/threads/774430-Receptor-Binding-affinity-meaning-and-units
“The affinity is measured by the concentration required to get 50% binding. If it is 5 nM for one compared to 50 uM for another, then it takes 10,000 times more ligand to get the same binding for the 50 uM compound as the 5 nM compound. However, the binding tells you nothing about the efficacy. The strongly bound compound could be a partial agonist and the weakly binding compound could be a full agonist, or vice versa. So, the 5 nM compound is stronger on a weight basis, but may not have stronger effects at equivalent doses.”
Recent AVXL News
- Anavex Life Sciences to Present at the H.C. Wainwright 26th Annual Global Investment Conference 2024 • GlobeNewswire Inc. • 09/03/2024 11:30:00 AM
- Form 10-Q - Quarterly report [Sections 13 or 15(d)] • Edgar (US Regulatory) • 08/06/2024 09:21:05 PM
- Anavex Life Sciences Reports Fiscal 2024 Third Quarter Financial Results and Provides Business Update • GlobeNewswire Inc. • 08/06/2024 11:30:00 AM
- Anavex Life Sciences to Announce Fiscal 2024 Third Quarter Financial Results on Tuesday, August 6, 2024 • GlobeNewswire Inc. • 08/01/2024 11:30:00 AM
- Form 8-K - Current report • Edgar (US Regulatory) • 07/30/2024 09:20:53 PM
- Anavex Life Sciences Announces Translational Biomarker Data for ANAVEX®2-73 (blarcamesine) in Fragile X Syndrome (Major Cause of Autism) at the 19th NFXF International Fragile X Conference • GlobeNewswire Inc. • 07/30/2024 11:30:00 AM
- Form S-3 - Registration statement under Securities Act of 1933 • Edgar (US Regulatory) • 07/29/2024 09:21:49 PM
- Results from Anavex Life Sciences Landmark Phase IIb/III Trial of Blarcamesine Presented at Alzheimer's Association Conference • GlobeNewswire Inc. • 07/28/2024 09:00:00 PM
- Anavex Life Sciences to Present at the H.C. Wainwright 5th Annual Neuro Perspectives Virtual Conference • GlobeNewswire Inc. • 06/20/2024 11:30:00 AM
- Form 4 - Statement of changes in beneficial ownership of securities • Edgar (US Regulatory) • 06/17/2024 11:30:10 AM
- Anavex Life Sciences Announces Expansion of Leadership Team • GlobeNewswire Inc. • 05/22/2024 11:30:00 AM
- Form 4 - Statement of changes in beneficial ownership of securities • Edgar (US Regulatory) • 05/17/2024 10:01:00 AM
- Anavex Life Sciences to Present at the H.C. Wainwright 2nd BioConnect Investor Conference at NASDAQ • GlobeNewswire Inc. • 05/14/2024 11:30:00 AM
- Shareholders that lost money on Anavex Life Sciences Corporation(AVXL) Urged to Join Class Action - Contact The Gross Law Firm to Learn More • PR Newswire (US) • 05/10/2024 09:45:00 AM
- Form 10-Q - Quarterly report [Sections 13 or 15(d)] • Edgar (US Regulatory) • 05/09/2024 08:35:55 PM
- Form 8-K - Current report • Edgar (US Regulatory) • 05/09/2024 12:00:30 PM
- Anavex Life Sciences Reports Fiscal 2024 Second Quarter Financial Results and Provides Business Update • GlobeNewswire Inc. • 05/09/2024 11:30:00 AM
- The Gross Law Firm Announces the Filing of a Securities Class Action on Behalf of Anavex Life Sciences Corporation(AVXL) Shareholders • PR Newswire (US) • 05/07/2024 09:45:00 AM
- Form DEFA14A - Additional definitive proxy soliciting materials and Rule 14(a)(12) material • Edgar (US Regulatory) • 05/06/2024 10:03:33 AM
- Anavex Life Sciences Corporation Sued for Securities Law Violations - Contact The Gross Law Firm Before May 13, 2024 to Discuss Your Rights - AVXL • PR Newswire (US) • 05/03/2024 09:45:00 AM
- Anavex Life Sciences to Announce Fiscal 2024 Second Quarter Financial Results on Thursday, May 9th, 2024 • GlobeNewswire Inc. • 05/02/2024 11:30:00 AM
- May 13, 2024 Deadline: Contact The Gross Law Firm to Join Class Action Suit Against AVXL • PR Newswire (US) • 04/26/2024 09:45:00 AM
- Contact The Gross Law Firm by May 13, 2024 Deadline to Join Class Action Against Anavex Life Sciences Corporation(AVXL) • PR Newswire (US) • 04/19/2024 09:45:00 AM
- The Gross Law Firm Reminds Shareholders of a Lead Plaintiff Deadline of May 13, 2024 in Anavex Life Sciences Lawsuit - AVXL • PR Newswire (US) • 04/16/2024 09:45:00 AM
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