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Restrict the search for
acetylcholine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
VU 10010 is a selective allosteric potentiator of M4 acetylcholine receptors. VU 10010 had no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5. VU 10010 is selective for M4 relative to other mAChRs - this compound does not displace [3H]NMS binding at any (rM1, rM2, rM3 and rM5) mAChR subtype. VU10010 was not found to be centrally active. It suffers from poor physiochemical properties. Novel analogs of VU10010 are CNS penetrant following systemic administration.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Sazetidine-A (6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol or AMOP-H-OH) is a "silent desensitizer" of neuronal nicotinic acetylcholine receptors (nAChRs), meaning that it desensitizes the receptor without first activating it. Later it was shown that Sazetidine-A is an agonist of native and recombinant alpha4beta2 nAChRs but shows differential efficacy on alpha4beta2 nAChRs subtypes. In animal models it is able to regulate the gain in body weight, alcohol and nicotine dependence. Sazetidine-A exerts analgesic, antidepressant and anxiolytic properties.
